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Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Abemaciclib [1231929-97-7]

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Referência HY-16297A-5mg

Tamanho : 5mg

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Marca : MedChemExpress

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Telefone : +1 850 650 7790

Description

Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

IC₅₀ & Target^[3]

Cdk4/cyclin D1

2 nM (IC₅₀)

CDK6/cyclinD1

10 nM (IC₅₀)

CDK9/cyclinT1

57 nM (IC₅₀)

CDK5/p35

287 nM (IC₅₀)

Cdk5/p25

355 nM (IC₅₀)

CDK2/cyclinE

504 nM (IC₅₀)

CDK1/cyclinB1

1627 nM (IC₅₀)

CDK7/Mat1/cyclinH1

3910 nM (IC₅₀)

PIM1

50 nM (IC₅₀)

PIM2

3400 nM (IC₅₀)

HIPK2

31 nM (IC₅₀)

DYRK2

61 nM (IC₅₀)

CK2

117 nM (IC₅₀)

GSK3b

192 nM (IC₅₀)

JNK3

389 nM (IC₅₀)

FLT3 (D835Y)

403 nM (IC₅₀)

DRAK1

659 nM (IC₅₀)

FLT3

3960 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A 172	EC₅₀	0.2 μM Compound: 3	Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
A549	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
BT-474	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human BT-474 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human BT-474 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
BXPC-3	IC₅₀	127 nM Compound: Abemaciclib	Antiproliferative activity against human BxPC3 cells Antiproliferative activity against human BxPC3 cells	[PMID: 31200237]
Calu-6	IC₅₀	17400 nM Compound: Chemical Probe: LY2835219	Cell cycle arrest in human Calu-6 cells assessed as reduction in pHH1 expression measured after 24 hrs by laser-scanning fluorescence cytometry Cell cycle arrest in human Calu-6 cells assessed as reduction in pHH1 expression measured after 24 hrs by laser-scanning fluorescence cytometry	[PMID: 24919854]
CFPAC-1	IC₅₀	371 nM Compound: Abemaciclib	Antiproliferative activity against human CFPAC-1 cells Antiproliferative activity against human CFPAC-1 cells	[PMID: 31200237]
COLO 205	EC₅₀	72 nM Compound: Chemical Probe: LY2835219	Cell cycle arrest in human COLO 205 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 24 hrs by propidium iodide staining based laser-scanning fluorescence cytometry Cell cycle arrest in human COLO 205 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 24 hrs by propidium iodide staining based laser-scanning fluorescence cytometry	[PMID: 24919854]
COLO 205	IC₅₀	0.217 μM Compound: Abemaciclib	Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay	[PMID: 29459274]
COLO 205	IC₅₀	0.46 μM Compound: LY2835219	Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay	[PMID: 29074254]
COLO 205	IC₅₀	120 nM Compound: LY-2835219	Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis	[PMID: 26115571]
COLO 205	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
COLO 205	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
CWR22R	GI₅₀	0.348 μM Compound: Abemaciclib	Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
DBTRG-05MG	EC₅₀	0.19 μM Compound: 3	Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
EMT6	IC₅₀	4.18 μM Compound: Abemaciclib	Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
HEK293	GI₅₀	10.925 μM Compound: Abemaciclib	Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HeLa	IC₅₀	768 nM Compound: Abemaciclib	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
HepG2	IC₅₀	216 nM Compound: Abemaciclib	Antiproliferative activity against human HepG2 cells Antiproliferative activity against human HepG2 cells	[PMID: 31200237]
HL-60	GI₅₀	0.664 μM Compound: Abemaciclib	Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HT-22	IC₅₀	12.2 μM Compound: 1	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
HUVEC	IC₅₀	403 nM Compound: Abemaciclib	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
Jurkat	GI₅₀	4.63 μM Compound: Abemaciclib	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
K562	GI₅₀	0.624 μM Compound: Abemaciclib	Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
K562	IC₅₀	1090 nM Compound: Abemaciclib	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 31200237]
LNCaP	IC₅₀	84 nM Compound: Abemaciclib	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 31200237]
M059J	EC₅₀	9.24 μM Compound: 3	Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
MCF-10A	GI₅₀	5.088 μM Compound: Abemaciclib	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	GI₅₀	0.832 μM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	GI₅₀	4.01 μM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MCF7	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human MCF7 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human MCF7 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
MCF7	IC₅₀	153 nM Compound: Abemacidib	Antiproliferative activity against Rb-proficient human MCF7 cells assessed as inhibition of cellular viability Antiproliferative activity against Rb-proficient human MCF7 cells assessed as inhibition of cellular viability	[PMID: 38670537]
MCF7	IC₅₀	7.29 μM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay	[PMID: 38283222]
MCF7	IC₅₀	99.8 nM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
MDA-MB-231	GI₅₀	3.45 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MDA-MB-231	IC₅₀	>20 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
MDA-MB-231	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
MDA-MB-231	IC₅₀	18.58 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay	[PMID: 38283222]
MDA-MB-231	IC₅₀	191 nM Compound: LY2835219	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay	[PMID: 29429832]
MDA-MB-231	IC₅₀	62 nM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
MDA-MB-361	EC₅₀	20 nM Compound: Chemical Probe: LY2835219	Cell cycle arrest in human MDA-MB-361 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 6 days by propidium iodide staining based laser-scanning fluorescence cytometry Cell cycle arrest in human MDA-MB-361 cells assessed as accumulation of cells at G1 phase by measuring increase in 2N DNA content measured after 6 days by propidium iodide staining based laser-scanning fluorescence cytometry	[PMID: 24919854]
MDA-MB-361	IC₅₀	90 nM Compound: Chemical Probe: LY2835219	Cytotoxicity against human MDA-MB-361 cells assessed as reduction in cell viability measured after 6 days Cytotoxicity against human MDA-MB-361 cells assessed as reduction in cell viability measured after 6 days	[PMID: 24919854]
MDA-MB-436	IC₅₀	1351 nM Compound: Abemacidib	Antiproliferative activity against Rb-deficient human MDA-MB-436 cells assessed as inhibition of cellular viability Antiproliferative activity against Rb-deficient human MDA-MB-436 cells assessed as inhibition of cellular viability	[PMID: 38670537]
MDA-MB-468	IC₅₀	>20 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
MDA-MB-468	IC₅₀	1144 nM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
MDA-MB-468	IC₅₀	4.808 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay	[PMID: 29459274]
MIA PaCa-2	IC₅₀	5.8 μM Compound: Abemaciclib	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 33316409]
NCI-H1975	IC₅₀	774 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-H1975 cells Antiproliferative activity against human NCI-H1975 cells	[PMID: 31200237]
NCI-H1993	IC₅₀	1156 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-H1993 cells Antiproliferative activity against human NCI-H1993 cells	[PMID: 31200237]
NCI-H358	IC₅₀	80.7 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-H358 cells Antiproliferative activity against human NCI-H358 cells	[PMID: 31200237]
NCI-H441	IC₅₀	263 nM Compound: Abemaciclib	Antiproliferative activity against human H441 cells Antiproliferative activity against human H441 cells	[PMID: 31200237]
NCI-N87	IC₅₀	519 nM Compound: Abemaciclib	Antiproliferative activity against human NCI-N87 cells Antiproliferative activity against human NCI-N87 cells	[PMID: 31200237]
Non-small cell lung cancer cell line	IC₅₀	0.7 μM Compound: 109	Antiproliferative activity against non-small cell lung cancer cell line (unknown origin) Antiproliferative activity against non-small cell lung cancer cell line (unknown origin)	[PMID: 33077264]
PANC-1	IC₅₀	701 nM Compound: Abemaciclib	Antiproliferative activity against human PANC1 cells Antiproliferative activity against human PANC1 cells	[PMID: 31200237]
PC-3	IC₅₀	9214 nM Compound: Abemaciclib	Antiproliferative activity against human PC3 cells Antiproliferative activity against human PC3 cells	[PMID: 31200237]
RPMI-8226	GI₅₀	1.479 μM Compound: Abemaciclib	Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
SF-539	EC₅₀	3.22 μM Compound: 3	Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
Sf9	IC₅₀	0.005 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.01 μM Compound: Abemaciclib	Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.065 μM Compound: Abemaciclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.101 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.273 μM Compound: Abemaciclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.347 μM Compound: Abemaciclib	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.371 μM Compound: Abemaciclib	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.371 μM Compound: LY2835219	Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP	[PMID: 26741853]
Sf9	IC₅₀	0.405 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	3.1 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
SiHa	IC₅₀	861 nM Compound: Abemaciclib	Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
SK-BR-3	IC₅₀	153 nM Compound: Abemaciclib	Antiproliferative activity against drug-sensitive human SK-BR-3 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against drug-sensitive human SK-BR-3 cells assessed as inhibition of cell growth by MTT assay	[PMID: 36893627]
SK-HEP1	IC₅₀	411 nM Compound: Abemaciclib	Antiproliferative activity against human SKHEP1 cells Antiproliferative activity against human SKHEP1 cells	[PMID: 31200237]
SNU-5	IC₅₀	523 nM Compound: Abemaciclib	Antiproliferative activity against human SNU5 cells Antiproliferative activity against human SNU5 cells	[PMID: 31200237]
T47D	GI₅₀	0.771 μM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
T47D	IC₅₀	145 nM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
T47D	IC₅₀	34.3 nM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
T98G	EC₅₀	0.54 μM Compound: 3	Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
THP-1	IC₅₀	187 nM Compound: Abemaciclib	Antiproliferative activity against human THP1 cells Antiproliferative activity against human THP1 cells	[PMID: 31200237]
U-251	IC₅₀	294 nM Compound: Abemaciclib	Antiproliferative activity against human U251 cells Antiproliferative activity against human U251 cells	[PMID: 31200237]
U-266	GI₅₀	2.701 μM Compound: Abemaciclib	Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
U-87MG ATCC	EC₅₀	0.12 μM Compound: 3	Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
U-87MG ATCC	IC₅₀	48.1 nM Compound: Amebaciclib	Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay	[PMID: 29247857]
U-87MG ATCC	IC₅₀	706 nM Compound: Abemaciclib	Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
U-87MG ATCC	IC₅₀	706 nM Compound: Abemaciclib	Antiproliferative activity against human U87MG cells Antiproliferative activity against human U87MG cells	[PMID: 31200237]
Vero	CC₅₀	>50 mM Compound: 16; LY2835219	Cytotoxicity against african green monkey Vero cells Cytotoxicity against african green monkey Vero cells	[PMID: 33970631]
Vero	CC₅₀	>50 μM Compound: Abemaciclib	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	6.62 μM Compound: Abemaciclib	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
ZR-75-1	IC₅₀	83.4 nM Compound: Abemaciclib	Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]

In Vitro

Abemaciclib reduces cell viability with the IC₅₀ values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells^[1]. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC₅₀ values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC₅₀ values of 395, 260, and 463 nM, respectively^[2]. Abemaciclib inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells^[3].

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

Solvant et solubilité

In Vitro:

DMSO : 2.94 mg/mL (5.80 mM; ultrasonic and warming and heat to 80°C; 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	1.9740 mL	9.8699 mL	19.7398 mL
5 mM	0.3948 mL	1.9740 mL	3.9480 mL
10 mM	---	---	---

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% Hydroxyethyl cellulose in Water
Solubility: 3.33 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Pureté et documentation

Purity: 99.97%

Fiche technique (278 KB) SDS (419 KB)

COA (244 KB) HNMR (232 KB) RP-HPLC (245 KB) MS (211 KB) Elemental Analysis Report (102 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13. [Content Brief]

[2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63. [Content Brief]

[3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37. [Content Brief]

[4]. Solmaz Sahebjam et al. Assessment of concentrations of abemaciclib and its major active metabolites in plasma, CSF, and brain tumor tissue in patients with brain metastases secondary to hormone receptor positive (HR+) breast cancer. J Clin Oncol 34. 2016, 526-526.

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NB-64-08240-1mg

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Referência HY-16297A-5mg

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Marca : MedChemExpress

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Abemaciclib Related Antibodies

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