Osimertinib [1421373-65-0]

Referência HY-15772-1mL

Tamanho : 10mM/1mL

Marca : MedChemExpress

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Telefone : +1 850 650 7790

Description

Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

IC50 & Target[1]

EGFRL858R

12 nM (IC50, Enzyme assays)

EGFRL858R/T790M

1 nM (IC50, Enzyme assays)

Cellular Effect
Cell Line Type Value Description References
A-431 CC50
550 nM
Compound: 6; AZD9291
Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay
Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay
[PMID: 36749735]
A-431 CC50
967 nM
Compound: Osimertinib
Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
[PMID: 31560541]
A-431 EC50
0.67 μM
Compound: Osimertinib
Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay
Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay
[PMID: 28853575]
A-431 EC50
0.7 μM
Compound: Osimertinib
Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
[PMID: 28603991]
A-431 EC50
0.956 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
[PMID: 35486541]
A-431 EC50
830 nM
Compound: 1
Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
[PMID: 37197473]
A-431 GI50
0.596 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
[PMID: 35486541]
A-431 GI50
40.1 nM
Compound: Osimertinib
Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
[PMID: 30442506]
A-431 GI50
619 nM
Compound: Osi; AZD9291
Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
A-431 IC50
0.4 μM
Compound: AZD9291
Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay
Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay
[PMID: 31889606]
A-431 IC50
0.61 μM
Compound: Osimertinib
Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
[PMID: 30442506]
A-431 IC50
0.619 μM
Compound: 6
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 37042119]
A-431 IC50
0.685 μM
Compound: AZD-9291
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
[PMID: 29534926]
A-431 IC50
0.77 μM
Compound: AZD9291
Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
A-431 IC50
0.77 μM
Compound: AZD9291
Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay
Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay
[PMID: 34534838]
A-431 IC50
0.821 μM
Compound: AZD9291
Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35447433]
A-431 IC50
0.821 μM
Compound: AZD9291
Cytotoxicity against human A-431 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human A-431 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
A-431 IC50
0.85 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
A-431 IC50
0.893 μM
Compound: AZD9291
Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay
Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay
[PMID: 27131639]
A-431 IC50
0.92 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
[PMID: 37885208]
A-431 IC50
0.945 μM
Compound: 6; AZD-9291
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
[PMID: 30471829]
A-431 IC50
0.956 μM
Compound: 3; AZD9291
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
[PMID: 28987609]
A-431 IC50
1.19 μM
Compound: 4
Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
[PMID: 31787359]
A-431 IC50
1.226 μM
Compound: AZD9291
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 34218082]
A-431 IC50
1.24 μM
Compound: AZD9291
Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay
Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay
[PMID: 30429956]
A-431 IC50
1.26 μM
Compound: 5; AZD9291
Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay
Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay
[PMID: 29730192]
A-431 IC50
1.3 μM
Compound: 4
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
[PMID: 31869655]
A-431 IC50
1.31 μM
Compound: 5; AZD9291
Antiproliferative activity against human A-431 cells by MTT assay
Antiproliferative activity against human A-431 cells by MTT assay
[PMID: 37336419]
A-431 IC50
1.325 μM
Compound: 4
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36288657]
A-431 IC50
1.4 μM
Compound: 2
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37839342]
A-431 IC50
1.44 μM
Compound: 4; AZD9291
Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay
Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay
[PMID: 31223440]
A-431 IC50
1.51 μM
Compound: 6, AZD9291
Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay
Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay
[PMID: 32631532]
A-431 IC50
1.604 μM
Compound: 3
Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay
Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay
[PMID: 28033579]
A-431 IC50
1310 nM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 35254067]
A-431 IC50
138.7 nM
Compound: AZD9291
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
[PMID: 33459024]
A-431 IC50
2.035 nM
Compound: 5
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 35446588]
A-431 IC50
2.64 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
[PMID: 38759458]
A-431 IC50
5.32 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33640672]
A-431 IC50
615.6 nM
Compound: AZD9291
Antiproliferative activity against human A431 cells harboring wild-type EGFR
Antiproliferative activity against human A431 cells harboring wild-type EGFR
[PMID: 28426996]
A-431 IC50
742 nM
Compound: AZD9291
Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
A-431 IC50
795.2 nM
Compound: AZD9291
Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
[PMID: 33667898]
A-431 IC50
795.2 μM
Compound: Osimertinib
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38879996]
A-431 IC50
84 nM
Compound: Osimertinib
Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
A549 EC50
1.83 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
[PMID: 28853575]
A549 GI50
3.5 μM
Compound: 5; AZD9291
Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
[PMID: 28282122]
A549 IC50
0.14 μM
Compound: AZD9291
Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay
Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay
[PMID: 31889606]
A549 IC50
0.31 μM
Compound: 2
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
[PMID: 30108918]
A549 IC50
0.335 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
[PMID: 34794818]
A549 IC50
0.445 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
[PMID: 35691176]
A549 IC50
0.462 μM
Compound: 3; AZD9291
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 31683104]
A549 IC50
0.53 μM
Compound: AZD
Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
[PMID: 29466773]
A549 IC50
0.53 μM
Compound: osimertinib
Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29853340]
A549 IC50
0.615 μM
Compound: 6; AZD9291
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 30530173]
A549 IC50
0.67 μM
Compound: AZD9291
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
A549 IC50
0.672 μM
Compound: AZD9291
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay
[PMID: 34534838]
A549 IC50
0.682 μM
Compound: 6
Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 37042119]
A549 IC50
0.72 μM
Compound: 4
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
[PMID: 31787359]
A549 IC50
0.784 μM
Compound: AZD9291
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35447433]
A549 IC50
0.86 μM
Compound: Osimertinib
Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay
Anticancer activity against human A549 cells incubated for 72 hrs by MTT assay
[PMID: 39094428]
A549 IC50
0.87 μM
Compound: AZD9291
Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay
Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay
[PMID: 29486953]
A549 IC50
0.9 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
A549 IC50
0.92 μM
Compound: Osimertinib
Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
A549 IC50
1.23 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
[PMID: 38759458]
A549 IC50
1.44 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38142512]
A549 IC50
1.557 nM
Compound: Osimertinib
Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
[PMID: 37087886]
A549 IC50
1.661 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 38169271]
A549 IC50
1.87 μM
Compound: 3
Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 35696862]
A549 IC50
1.87 μM
Compound: Osimertinib
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38879996]
A549 IC50
1.97 μM
Compound: Osimertinib
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
[PMID: 32961382]
A549 IC50
150 nM
Compound: 9; AZD9291
Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
[PMID: 26756222]
A549 IC50
2.67 μM
Compound: Osimertinib
Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
A549 IC50
3.242 μM
Compound: 6; AZD-9291
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 30471829]
A549 IC50
486 nM
Compound: AZD9291
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 29576272]
A549 IC50
5 μM
Compound: Osimertinib
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
A549 IC50
9.4 μM
Compound: OSI
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 37141440]
ASPC1 IC50
3.985 μM
Compound: 6; AZD-9291
Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay
Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay
[PMID: 30471829]
BaF3 CC50
14 nM
Compound: 6; AZD9291
Antiproliferative activity against mouse BaF3 cells overexpressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 96 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells overexpressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 96 hrs by MTS assay
[PMID: 36749735]
BaF3 EC50
>5000 nM
Compound: Osimertinib
Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
>5 μM
Compound: Osimertinib
Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
0.545 μM
Compound: Osimertinib
Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
[PMID: 35486541]
BaF3 EC50
14 nM
Compound: AZD9291
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay
[PMID: 36518696]
BaF3 EC50
16 nM
Compound: Osimertinib
Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
1748 nM
Compound: Osimertinib
Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
18 nM
Compound: Osimertinib
Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
20 nM
Compound: Osimertinib
Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
2956 nM
Compound: 1
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
[PMID: 37197473]
BaF3 EC50
3.2 nM
Compound: AZD9291
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay
[PMID: 36518696]
BaF3 EC50
34 nM
Compound: AZD9291
Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay
Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay
[PMID: 36518696]
BaF3 EC50
6 nM
Compound: 1
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
[PMID: 37197473]
BaF3 EC50
6 nM
Compound: Osimertinib
Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 EC50
66 nM
Compound: Osimertinib
Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28528303]
BaF3 GI50
0.347 μM
Compound: Osimertinib
Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
[PMID: 35486541]
BaF3 GI50
1.2 μM
Compound: 5; AZD9291
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
[PMID: 28282122]
BaF3 GI50
107 nM
Compound: 1
Inhibition of cell proliferation of mouse BaF3 cells expressing wild-type EGFR (unknown origin)
Inhibition of cell proliferation of mouse BaF3 cells expressing wild-type EGFR (unknown origin)
[PMID: 38065292]
BaF3 GI50
1288 nM
Compound: 1
Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant (unknown origin)
Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant (unknown origin)
[PMID: 38065292]
BaF3 GI50
14 nM
Compound: Osi; AZD9291
Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
BaF3 GI50
179 nM
Compound: Osi; AZD9291
Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
BaF3 GI50
2065 nM
Compound: 1
Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR Del19/T790M/C797S mutant (unknown origin)
Inhibition of cell proliferation of mouse BaF3 cells expressing EGFR Del19/T790M/C797S mutant (unknown origin)
[PMID: 38065292]
BaF3 GI50
299 nM
Compound: Osi; AZD9291
Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
BaF3 GI50
376 nM
Compound: Osi; AZD9291
Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
BaF3 IC50
>1 μM
Compound: 65, AZD9291
Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
[PMID: 26258521]
BaF3 IC50
>3000 nM
Compound: 4
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
[PMID: 34464874]
BaF3 IC50
>3 μM
Compound: 4
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
[PMID: 34464874]
BaF3 IC50
0.009 μM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring wildtype EGFR assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring wildtype EGFR assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 38142512]
BaF3 IC50
0.033 μM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 36064123]
BaF3 IC50
0.75 μM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring EGFR Del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR Del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 38142512]
BaF3 IC50
0.859 μM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 36064123]
BaF3 IC50
1 nM
Compound: Osimertinib
Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
BaF3 IC50
1.12 μM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 38142512]
BaF3 IC50
1.634 μM
Compound: OSI
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 37141440]
BaF3 IC50
10.1 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
110 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
1100 nM
Compound: Osimertinib
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
BaF3 IC50
1200 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
1320.5 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
1409.5 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
1475 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
1503.9 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
154.1 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
16 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
19 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring EGFR-L858R/C775S mutant assessed as inhibition of cell proliferation measured after 3 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR-L858R/C775S mutant assessed as inhibition of cell proliferation measured after 3 days by CellTiter-Glo assay
[PMID: 38300264]
BaF3 IC50
2 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
2.5 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
2.885 μM
Compound: AZD9291; 5
Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
[PMID: 35178175]
BaF3 IC50
2.893 μM
Compound: AZD9291; 5
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
[PMID: 35178175]
BaF3 IC50
21.5 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
[PMID: 33459024]
BaF3 IC50
3 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
3.3 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
3.38 μM
Compound: 5
Cytotoxicity against mouse BaF3 cells harboring EGFR-Del19/T790M/C797S mutant assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against mouse BaF3 cells harboring EGFR-Del19/T790M/C797S mutant assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay
[PMID: 36417820]
BaF3 IC50
3.52 μM
Compound: 5
Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35446588]
BaF3 IC50
3.93 μM
Compound: 4; AZD9291
Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
[PMID: 31223440]
BaF3 IC50
300.1 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
3100 nM
Compound: Osimertinib
Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
[PMID: 31689114]
BaF3 IC50
350.5 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay
[PMID: 37669428]
BaF3 IC50
4 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
[PMID: 33459024]
BaF3 IC50
4.14 μM
Compound: 5
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by resazurin dye-based fluorescence assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by resazurin dye-based fluorescence assay
[PMID: 36417820]
BaF3 IC50
4.27 μM
Compound: 5
Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35446588]
BaF3 IC50
4.3 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
4.427 μM
Compound: AZD9291; 5
Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
[PMID: 35178175]
BaF3 IC50
4.484 μM
Compound: OSI
Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 37141440]
BaF3 IC50
4.5 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
4.61 μM
Compound: AZD9291
Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay
Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay
[PMID: 30429956]
BaF3 IC50
5.11 μM
Compound: 4; AZD9291
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
[PMID: 31223440]
BaF3 IC50
5.15 μM
Compound: AZD9291
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay
[PMID: 30429956]
BaF3 IC50
5.47 μM
Compound: 6, AZD9291
Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay
Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay
[PMID: 32631532]
BaF3 IC50
53.1 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
57 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay
[PMID: 37669428]
BaF3 IC50
6.071 nM
Compound: 5
Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 35446588]
BaF3 IC50
60.6 nM
Compound: Osimertinib
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
752.4 nM
Compound: Osimertinib
Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
BaF3 IC50
780 nM
Compound: Osimertinib
Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
BaF3 IC50
8 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
800 nM
Compound: AZD9291
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
[PMID: 34668706]
BaF3 IC50
81 nM
Compound: Osimertinib
Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
BC IC50
0.015 μM
Compound: 58; AZD9291
Inhibition of cell growth in human multiple BC cells bearing EZH2 T790M mutant
Inhibition of cell growth in human multiple BC cells bearing EZH2 T790M mutant
[PMID: 35093670]
BC IC50
0.015 μM
Compound: 58; AZD9291
Inhibition of cell growth in human multiple BC cells bearing wildtype EZH2
Inhibition of cell growth in human multiple BC cells bearing wildtype EZH2
[PMID: 35093670]
BEAS-2B IC50
14.9 μM
Compound: 1; AZD9291
Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay
Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay
[PMID: 28716641]
BJ IC50
>10 μM
Compound: AZD9291
Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
Calu-3 GI50
264 nM
Compound: 8
Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
[PMID: 25271963]
Calu-3 IC50
0.75 μM
Compound: Osimertinib
Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay
Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay
[PMID: 30442506]
Calu-6 IC50
5.86 μM
Compound: Osimertinib
Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay
Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay
[PMID: 30442506]
CHO GI50
4.2 μM
Compound: 5; AZD9291
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
[PMID: 28282122]
CL97 IC50
0.1 μM
Compound: Osimertinib
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
EA.hy 926 IC50
1.161 μM
Compound: Osimertinib
Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
[PMID: 37087886]
HaCaT IC50
3.356 μM
Compound: Osi
Cytotoxicity against human HaCaT cells
Cytotoxicity against human HaCaT cells
[PMID: 38908104]
HaCaT IC50
73.7 nM
Compound: 5; AZD9291
Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
[PMID: 27433829]
HCC827 EC50
<0.014 μM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
[PMID: 28853575]
HCC827 GI50
4.5 nM
Compound: Osi; AZD9291
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
HCC827 IC50
0.001 μM
Compound: 2
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37839342]
HCC827 IC50
0.001 μM
Compound: 5; AZD9291
Antiproliferative activity against human HCC827 cells by MTT assay
Antiproliferative activity against human HCC827 cells by MTT assay
[PMID: 37336419]
HCC827 IC50
0.00173 μM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay
[PMID: 34794818]
HCC827 IC50
0.00248 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
[PMID: 35691176]
HCC827 IC50
0.003 μM
Compound: 4
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
[PMID: 31787359]
HCC827 IC50
0.003 μM
Compound: 6
Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 37042119]
HCC827 IC50
0.004 μM
Compound: Osimertinib
Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
HCC827 IC50
0.006 μM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
[PMID: 38759458]
HCC827 IC50
0.007 μM
Compound: Osimertinib
Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay
Anticancer activity against human HCC827 cells incubated for 72 hrs by MTT assay
[PMID: 39094428]
HCC827 IC50
0.011 μM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay
Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay
[PMID: 30442506]
HCC827 IC50
0.016 μM
Compound: AZD9291
Cytotoxicity against human HCC827 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human HCC827 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
HCC827 IC50
0.027 μM
Compound: AZD
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
[PMID: 29466773]
HCC827 IC50
0.027 μM
Compound: osimertinib
Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay
[PMID: 29853340]
HCC827 IC50
0.03 μM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 38169271]
HCC827 IC50
0.036 μM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
HCC827 IC50
0.057 μM
Compound: OS
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
[PMID: 37870244]
HCC827 IC50
0.2 μM
Compound: AZD9291
Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay
Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay
[PMID: 31889606]
HCC827 IC50
0.97 nM
Compound: AZD9291
Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
HCC827 IC50
1 nM
Compound: Osimertinib
Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 35254067]
HCC827 IC50
25.4 nM
Compound: AZD9291
Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay
[PMID: 29576272]
HCC827 IC50
32.31 nM
Compound: AZD9291
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
[PMID: 37356356]
HCC827 IC50
33.7 nM
Compound: AZD9291
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
[PMID: 37356356]
HCC827 IC50
61.6 nM
Compound: AZD9291
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant
[PMID: 28426996]
HEK293 IC50
0.57 μM
Compound: AZD9291
Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis
Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis
[PMID: 28426996]
HEK293-A IC50
2.418 μM
Compound: AZD9291
Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
HeLa IC50
0.975 μM
Compound: 3; AZD9291
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 31683104]
HeLa IC50
1.83 μM
Compound: AZD9291
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
HepG2 IC50
1.605 μM
Compound: 6; AZD9291
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 30530173]
HepG2 IC50
3.06 μM
Compound: 2
Antiproliferative activity against human HepG2 cells harboring VEGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells harboring VEGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37839342]
HK-2 IC50
2.138 μM
Compound: Osi
Cytotoxicity against human HK-2 cells
Cytotoxicity against human HK-2 cells
[PMID: 38908104]
HK-2 IC50
2.399 μM
Compound: Osimertinib
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
[PMID: 37087886]
HK-2 IC50
2.719 μM
Compound: AZD9291
Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay
[PMID: 33429247]
HK-2 IC50
3.565 μM
Compound: AZD9291
Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
HT-29 IC50
0.65 μM
Compound: AZD9291
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 29486953]
HUVEC IC50
2.399 μM
Compound: Osi
Cytotoxicity against human HUVEC cells
Cytotoxicity against human HUVEC cells
[PMID: 38908104]
HUVEC IC50
2.399 μM
Compound: Osi
Cytotoxicity against VEGF-stimulated human HUVEC cells
Cytotoxicity against VEGF-stimulated human HUVEC cells
[PMID: 38908104]
HUVEC IC50
7.278 μM
Compound: AZD9291
Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 32619886]
KG-1 IC50
0.53 μM
Compound: Osimertinib
Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay
[PMID: 32961382]
L02 IC50
>40 μM
Compound: Osimertinib
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33640672]
L02 IC50
>50 μM
Compound: AZD9291
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
L02 IC50
0.3 μM
Compound: AZD9291
Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay
Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay
[PMID: 31889606]
L02 IC50
1.602 μM
Compound: AZD9291
Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
L02 IC50
1.955 μM
Compound: Osi
Cytotoxicity against human L02 cells
Cytotoxicity against human L02 cells
[PMID: 38908104]
L02 IC50
1.975 μM
Compound: AZD9291
Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay
[PMID: 33429247]
L02 IC50
8.42 μM
Compound: Osimertinib
Cytotoxicity against human L02 cells assessed as inhibition of cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell viability measured after 72 hrs by MTT assay
[PMID: 38169271]
LoVo IC50
480 nM
Compound: AZD9291
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
[PMID: 26968253]
LoVo IC50
480 μM
Compound: 8
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
[PMID: 25271963]
LoVo IC50
480 nM
Compound: Osimertinib
Antiproliferative activity against human LoVo cells harboring wild-type EGFR assessed as reduction in cell viability
Antiproliferative activity against human LoVo cells harboring wild-type EGFR assessed as reduction in cell viability
[PMID: 38879996]
Lymphoma cell line IC50
0.015 μM
Compound: 58; AZD9291
Inhibition of cell growth in human Lymphoma cell line bearing EZH2 T790M mutant
Inhibition of cell growth in human Lymphoma cell line bearing EZH2 T790M mutant
[PMID: 35093670]
Lymphoma cell line IC50
0.015 μM
Compound: 58; AZD9291
Inhibition of cell growth in human Lymphoma cell line bearing wildtype EZH2
Inhibition of cell growth in human Lymphoma cell line bearing wildtype EZH2
[PMID: 35093670]
MCF7 IC50
1.16 μM
Compound: Osimertinib
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
[PMID: 38323982]
MCF7 IC50
3.525 μM
Compound: AZD9291
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
MCF7 IC50
3.67 μM
Compound: AZD9291
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 32679450]
MDA-MB-231 IC50
2.25 μM
Compound: AZD9291
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 36762554]
MDA-MB-468 IC50
1.3 μM
Compound: Osimertinib
Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay
[PMID: 32961382]
NCI-H1299 IC50
>10 μM
Compound: AZD9291; 5
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
[PMID: 35178175]
NCI-H1299 IC50
2.84 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
[PMID: 34794818]
NCI-H1299 IC50
3.24 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
[PMID: 35691176]
NCI-H1975 CC50
43 nM
Compound: 6; AZD9291
Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay
[PMID: 36749735]
NCI-H1975 EC50
<0.014 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
[PMID: 28853575]
NCI-H1975 EC50
0.019 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
[PMID: 28603991]
NCI-H1975 GI50
2.8 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
[PMID: 30442506]
NCI-H1975 GI50
24 nM
Compound: 8
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
[PMID: 25271963]
NCI-H1975 GI50
35 nM
Compound: Osi; AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
NCI-H1975 IC50
<1 μM
Compound: 4
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay
[PMID: 31869655]
NCI-H1975 IC50
0.004 μM
Compound: Osimertinib
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
[PMID: 38879996]
NCI-H1975 IC50
0.007 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
[PMID: 37885208]
NCI-H1975 IC50
0.011 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
[PMID: 33429247]
NCI-H1975 IC50
0.012 μM
Compound: 4
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
[PMID: 31787359]
NCI-H1975 IC50
0.013 μM
Compound: 2
Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
[PMID: 30108918]
NCI-H1975 IC50
0.014 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
NCI-H1975 IC50
0.0148 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
[PMID: 34794818]
NCI-H1975 IC50
0.015 μM
Compound: 6
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 37042119]
NCI-H1975 IC50
0.015 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
[PMID: 38323982]
NCI-H1975 IC50
0.016 μM
Compound: 1
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay
[PMID: 32550993]
NCI-H1975 IC50
0.019 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
[PMID: 37087886]
NCI-H1975 IC50
0.019 μM
Compound: AZD
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
[PMID: 29466773]
NCI-H1975 IC50
0.019 μM
Compound: osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
[PMID: 29853340]
NCI-H1975 IC50
0.022 μM
Compound: AZD9291
Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
NCI-H1975 IC50
0.022 μM
Compound: OSI
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 37141440]
NCI-H1975 IC50
0.023 μM
Compound: AZD-9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
[PMID: 29534926]
NCI-H1975 IC50
0.03 μM
Compound: 3
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay
[PMID: 28033579]
NCI-H1975 IC50
0.03 μM
Compound: 4; AZD9291
Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay
Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay
[PMID: 31223440]
NCI-H1975 IC50
0.03 μM
Compound: 2
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37839342]
NCI-H1975 IC50
0.0305 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
[PMID: 35691176]
NCI-H1975 IC50
0.04 μM
Compound: Osimertinib
Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
NCI-H1975 IC50
0.041 μM
Compound: 5; AZD9291
Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay
Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay
[PMID: 29730192]
NCI-H1975 IC50
0.044 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
NCI-H1975 IC50
0.05 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
NCI-H1975 IC50
0.052 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay
[PMID: 27131639]
NCI-H1975 IC50
0.06 μM
Compound: AZD9291
Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay
Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay
[PMID: 29486953]
NCI-H1975 IC50
0.06 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
[PMID: 30442506]
NCI-H1975 IC50
0.064 μM
Compound: 3; AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
[PMID: 28987609]
NCI-H1975 IC50
0.07 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay
[PMID: 31718182]
NCI-H1975 IC50
0.072 μM
Compound: 3
Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 35696862]
NCI-H1975 IC50
0.073 μM
Compound: 3; AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 31683104]
NCI-H1975 IC50
0.073 μM
Compound: 6; AZD9291
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
[PMID: 30530173]
NCI-H1975 IC50
0.076 μM
Compound: AZD9291
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay
[PMID: 34534838]
NCI-H1975 IC50
0.081 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 38169271]
NCI-H1975 IC50
0.091 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 34218082]
NCI-H1975 IC50
0.095 μM
Compound: 4
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay
[PMID: 36288657]
NCI-H1975 IC50
0.096 μM
Compound: 6; AZD-9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay
[PMID: 30471829]
NCI-H1975 IC50
0.1 μM
Compound: 4
Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay
Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay
[PMID: 30472599]
NCI-H1975 IC50
0.1 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 35178185]
NCI-H1975 IC50
0.11 μM
Compound: OS
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
[PMID: 37870244]
NCI-H1975 IC50
0.125 μM
Compound: 1
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36173763]
NCI-H1975 IC50
0.13 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay
[PMID: 30429956]
NCI-H1975 IC50
0.13 μM
Compound: 5; AZD9291
Antiproliferative activity against human NCI-H1975 cells by MTT assay
Antiproliferative activity against human NCI-H1975 cells by MTT assay
[PMID: 37336419]
NCI-H1975 IC50
0.32 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38142512]
NCI-H1975 IC50
0.63 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay
[PMID: 38759458]
NCI-H1975 IC50
0.74 μM
Compound: 6, AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay
[PMID: 32631532]
NCI-H1975 IC50
0.98 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33640672]
NCI-H1975 IC50
1.3 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 36762554]
NCI-H1975 IC50
1.51 μM
Compound: 7
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38401457]
NCI-H1975 IC50
10.5 nM
Compound: 1; AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay
[PMID: 28716641]
NCI-H1975 IC50
15 nM
Compound: 9; AZD9291
Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA
Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA
[PMID: 26756222]
NCI-H1975 IC50
15 μM
Compound: 8
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
[PMID: 25271963]
NCI-H1975 IC50
15 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
[PMID: 35254067]
NCI-H1975 IC50
15 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 38879996]
NCI-H1975 IC50
15 μM
Compound: 8
Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
[PMID: 25271963]
NCI-H1975 IC50
17 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 35254067]
NCI-H1975 IC50
18.21 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
[PMID: 33667898]
NCI-H1975 IC50
18.21 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo assay
[PMID: 38879996]
NCI-H1975 IC50
2.08 μM
Compound: Osimertinib
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay
[PMID: 33640672]
NCI-H1975 IC50
2.94 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 38142512]
NCI-H1975 IC50
2327 nM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cell assessed as cell growth inhibition
Antiproliferative activity against human NCI-H1975 cell assessed as cell growth inhibition
[PMID: 38838547]
NCI-H1975 IC50
3 μM
Compound: 17
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability
[PMID: 38043489]
NCI-H1975 IC50
3.1 μM
Compound: Osimertinib
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay
[PMID: 31718182]
NCI-H1975 IC50
3.85 μM
Compound: 1
Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36173763]
NCI-H1975 IC50
4.32 μM
Compound: 1
Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36173763]
NCI-H1975 IC50
4.69 μM
Compound: OS
Antiproliferative activity against human Osimertinib-resistant NCI-H1975 cell incubated for 72 hrs by MTT assay
Antiproliferative activity against human Osimertinib-resistant NCI-H1975 cell incubated for 72 hrs by MTT assay
[PMID: 37870244]
NCI-H1975 IC50
42 nM
Compound: AZD9291
Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
NCI-H1975 IC50
43.63 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
[PMID: 37356356]
NCI-H1975 IC50
44.61 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
[PMID: 37356356]
NCI-H1975 IC50
47.2 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
[PMID: 29576272]
NCI-H1975 IC50
47.3 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
[PMID: 33459024]
NCI-H1975 IC50
67 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant
[PMID: 28426996]
NCI-H1975 IC50
73.4 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
[PMID: 32679450]
NCI-H292 IC50
0.22 μM
Compound: 1
Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay
Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay
[PMID: 32550993]
NCI-H292 IC50
0.924 nM
Compound: AZD9291
Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay
Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay
[PMID: 33429247]
NCI-H292 IC50
1.084 μM
Compound: AZD9291
Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
NCI-H292 IC50
2 μM
Compound: Osimertinib
Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
[PMID: 38879996]
NCI-H460 IC50
415.9 nM
Compound: 1; AZD9291
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay
[PMID: 28716641]
Non-small cell lung cancer cell line IC50
41 nM
Compound: Osimertinib
Antiproliferative activity against Non-small cell lung cancer cells (unknown origin)
Antiproliferative activity against Non-small cell lung cancer cells (unknown origin)
[PMID: 38432059]
PC-9 GI50
23 nM
Compound: 8
Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
[PMID: 25271963]
PC-9 GI50
6.7 nM
Compound: Osi; AZD9291
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 37406381]
PC-9 IC50
<0.01 μM
Compound: Osimertinib
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
PC-9 IC50
>1000 nM
Compound: Osimertinib
Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
PC-9 IC50
>1 μM
Compound: Osimertinib
Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 31689114]
PC-9 IC50
0.005 μM
Compound: Osimertinib
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
[PMID: 37885208]
PC-9 IC50
0.005 μM
Compound: Osimertinib
Cytotoxicity against human PC-9 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human PC-9 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
[PMID: 38879996]
PC-9 IC50
0.011 nM
Compound: AZD9291
Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay
Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay
[PMID: 33429247]
PC-9 IC50
0.011 μM
Compound: AZD9291; 5
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
[PMID: 35178175]
PC-9 IC50
0.015 μM
Compound: AZD9291
Cytotoxicity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
PC-9 IC50
0.016 μM
Compound: AZD9291
Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31581004]
PC-9 IC50
0.021 μM
Compound: OSI
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 37141440]
PC-9 IC50
0.023 nM
Compound: Osimertinib
Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
[PMID: 37087886]
PC-9 IC50
0.08 μM
Compound: 5
Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 36417820]
PC-9 IC50
0.16 μM
Compound: Osimertinib
Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay
Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay
[PMID: 30442506]
PC-9 IC50
11.31 nM
Compound: Osimertinib
Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
PC-9 IC50
17 nM
Compound: AZD9291
Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
[PMID: 26968253]
PC-9 IC50
17 μM
Compound: 8
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
[PMID: 25271963]
PC-9 IC50
17 nM
Compound: Osimertinib
Antiproliferative activity against human PC-9 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation
Antiproliferative activity against human PC-9 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation
[PMID: 35254067]
PC-9 IC50
17 nM
Compound: Osimertinib
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
[PMID: 38879996]
PC-9 IC50
2.2 μM
Compound: Osimertinib
Antiproliferative activity against human PC-9 cells harbouring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
Antiproliferative activity against human PC-9 cells harbouring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
[PMID: 37885208]
PC-9 IC50
2.789 μM
Compound: AZD9291
Cytotoxicity against human PC-9 cells expressing EGFR Del19/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human PC-9 cells expressing EGFR Del19/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
PC-9 IC50
3.21 μM
Compound: AZD9291; 5
Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
[PMID: 35178175]
PC-9 IC50
3.248 μM
Compound: AZD9291
Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35447433]
PC-9 IC50
3.248 μM
Compound: AZD9291
Cytotoxicity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
Cytotoxicity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
[PMID: 39094277]
PC-9 IC50
3461 nM
Compound: Osimertinib
Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
PC-9 IC50
4.85 μM
Compound: 5
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36417820]
PC-9 IC50
5.431 nM
Compound: 5
Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 35446588]
PC-9 IC50
56 nM
Compound: 9; AZD9291
Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
[PMID: 26756222]
PC-9 IC50
6.5 nM
Compound: 1; AZD9291
Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay
Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay
[PMID: 28716641]
PC-9 IC50
7.463 nM
Compound: Osimertinib
Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
Sf9 IC50
0.002 μM
Compound: Osimertinib
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k
[PMID: 31718182]
Sf9 IC50
0.09 μM
Compound: Osimertinib
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki
[PMID: 31718182]
Sf9 IC50
1.23 μM
Compound: Osimertinib
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
[PMID: 31718182]
Sf9 IC50
20.8 nM
Compound: 6; AZD-9291
Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
[PMID: 30471829]
Sf9 IC50
567.5 nM
Compound: 6; AZD-9291
Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
[PMID: 30471829]
U-87MG ATCC IC50
4.5 μM
Compound: 4
Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
[PMID: 31869655]
Vero CC50
13.23 μM
Compound: Osimertinib
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
3.26 μM
Compound: Osimertinib
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
In Vitro

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
? Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].
? Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)[2].
? Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively)[1].
? Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferation (IC50s=6, 7, 74 nM, respectively)

Cell Proliferation Assay[2]

Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Dramatically inhibited cell proliferation (IC50s=41, 26, 41, 31 nM, respectively)

Cell Proliferation Assay[2]

Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferation (IC50s=16, 701, 230, 38 nM, respectively)

Apoptosis Analysis[2]

Cell Line: Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.
In Vivo

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration: p.o.; daily for 14 days
Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
Essai clinique
Masse moléculaire

499.61

Formule

C28H33N7O2

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (200.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0016 mL 10.0078 mL 20.0156 mL
5 mM 0.4003 mL 2.0016 mL 4.0031 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

Pureté et documentation
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