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

Palbociclib [571190-30-2]

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Referência HY-50767-10mg

Tamanho : 10mg

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Marca : MedChemExpress

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Telefone : +1 850 650 7790

Description

Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma^[1]^[3]^[4].

IC₅₀ & Target^[1]

Cdk4/cyclin D3

9 nM (IC₅₀)

Cdk4/cyclin D1

11 nM (IC₅₀)

Cdk6/cyclin D2

16 nM (IC₅₀)

DYRK1A

2000 nM (IC₅₀)

MAPK

8000 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	0.032 μM Compound: Palbociclib	Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
A-375	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
A549	EC₅₀	0.4 μM Compound: Palbociclib	Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
A549	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
A549	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
A549	IC₅₀	1.32 μM Compound: V	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
A549	IC₅₀	8.07 μM Compound: Palbociclib	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: 37011445]
A549	IC₅₀	9.4 μM Compound: Palbociclib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
B16-F10	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
BPH-1	GI₅₀	7.442 μM Compound: Palbociclib	Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
Calu-1	EC₅₀	33 μM Compound: Palbociclib	Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
COLO 205	IC₅₀	0.036 μM Compound: Palbociclib	Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
COLO 205	IC₅₀	300.6 nM Compound: Palbociclib	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	0.435 μM Compound: Palbociclib	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]
DU-145	GI₅₀	5.792 μM Compound: Palbociclib	Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
DU-145	IC₅₀	7.5 μM Compound: 31, PD-0332991	Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 24417566]
HCC38	EC₅₀	1.4 μM Compound: 51	Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
HCT-116	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
HCT-116	IC₅₀	7.11 μM Compound: 1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HCT-116	IC₅₀	8.9 μM Compound: V	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
HEK293	GI₅₀	9.608 μM Compound: Palbociclib	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	>10 μM Compound: Palbociclib	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
HeLa	IC₅₀	13.3 μM Compound: 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HepG2	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
HepG2	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
HepG2	IC₅₀	9.92 μM Compound: Palbociclib	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
HL-60	GI₅₀	29.17 μM Compound: Palbociclib	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34958208]
HL-60	GI₅₀	3.498 μM Compound: Palbociclib	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-29	IC₅₀	3.56 μM Compound: 1	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
HT-29	IC₅₀	9.3 μM Compound: Palbociclib	Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay	[PMID: 36130661]
JeKo-1	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
Jurkat	GI₅₀	>100 μM Compound: Palbociclib	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]
Jurkat	IC₅₀	1.495 μM Compound: Palbociclib	Anti-proliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Anti-proliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 38943626]
K562	GI₅₀	2.455 μM Compound: Palbociclib	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	>10 μM Compound: Palbociclib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
K562	IC₅₀	2 μM Compound: 31, PD-0332991	Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 24417566]
L02	GI₅₀	>100 μM Compound: Palbociclib	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
L02	IC₅₀	25.63 μM Compound: Pal	Cytotoxicity against human L02 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
L02	IC₅₀	34.12 μM Compound: Pal	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
LNCaP C4-2B	GI₅₀	4.15 μM Compound: Palbociclib	Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MCF-10A	GI₅₀	19.07 μM Compound: Palbociclib	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	>100 μM Compound: Palbociclib	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	GI₅₀	0.557 μM Compound: Palbociclib	Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MCF7	GI₅₀	3.938 μM Compound: Palbociclib	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	IC₅₀	>10 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34624191]
MCF7	IC₅₀	0.34 μM Compound: PD0332991	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MCF7	IC₅₀	0.78 μM Compound: Palbociclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MCF7	IC₅₀	240 nM Compound: 1	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MCF7	IC₅₀	4.09 μM Compound: V	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MCF7	IC₅₀	5.81 μM Compound: Palbociclib	Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MCF7	IC₅₀	6.21 μM Compound: Palbociclib	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	85.2 nM Compound: Palbociclib	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]
MDA-MB-231	EC₅₀	0.3 μM Compound: 51	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
MDA-MB-231	GI₅₀	>100 μM Compound: Palbociclib	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	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	IC₅₀	>10 μM Compound: Palbociclib	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
MDA-MB-231	IC₅₀	14.6 μM Compound: Paldociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	3.5 μM Compound: V	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MDA-MB-231	IC₅₀	4.72 μM Compound: PD0332991	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MDA-MB-231	IC₅₀	5.22 μM Compound: Palbociclib	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	5.62 μM Compound: Palbociclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37011445]
MDA-MB-231	IC₅₀	580 nM Compound: 1	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MDA-MB-231	IC₅₀	6.21 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 33197548]
MDA-MB-435	IC₅₀	0.16 μM Compound: 43(table 3)	Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line	[PMID: 15801831]
MDA-MB-435	IC₅₀	160 nM Compound: PD-0332991	Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis	[PMID: 26115571]
MDA-MB-436	EC₅₀	5 μM Compound: 51	Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis	[PMID: 33650861]
MDA-MB-436	IC₅₀	>10000 nM Compound: Palbociclib	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-453	GI₅₀	0.326 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay	[PMID: 28156111]
MDA-MB-453	IC₅₀	137 nM Compound: 1	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 27448913]
MDA-MB-453	IC₅₀	6.93 μM Compound: PD0332991	Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
MDA-MB-468	EC₅₀	1.9 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
MDA-MB-468	GI₅₀	5.96 μM Compound: Palbociclib	Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MDA-MB-468	IC₅₀	>3 μM Compound: 43(table 3)	Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line	[PMID: 15801831]
MDA-MB-468	IC₅₀	>3 μM Compound: PD-0332991	Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis	[PMID: 26115571]
MDA-MB-468	IC₅₀	5424 nM Compound: Palbociclib	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]
MIA PaCa-2	IC₅₀	10.6 μM Compound: Palbociclib	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]
MM1.S	IC₅₀	200 nM Compound: PD	Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay	[PMID: 31330105]
MOLM-13	GI₅₀	>80 μM Compound: Palbociclib	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34958208]
MOLM-13	GI₅₀	0.062 μM Compound: Palbociclib	Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MOLM-13	IC₅₀	>3 μM Compound: Palbociclib	Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs	[PMID: 24641103]
MOLM-13	IC₅₀	0.011 μM Compound: Palbociclib	Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs	[PMID: 24641103]
MOLM-13	IC₅₀	0.096 μM Compound: Palbociclib	Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
MOLM-13	IC₅₀	0.096 μM Compound: Palbociclib	Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
MRC5	GI₅₀	>10 μM Compound: Palbociclib	Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
MV4-11	GI₅₀	0.05 μM Compound: Palbociclib	Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay	[PMID: 28156111]
NB-4	GI₅₀	0.066 μM Compound: Palbociclib	Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
NCI-H1299	IC₅₀	0.27 μM Compound: Pal	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H1299	IC₅₀	0.31 μM Compound: Pal	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H1299	IC₅₀	8.92 μM Compound: PD0332991	Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33857728]
NCI-H2228	IC₅₀	1.42 μM Compound: Pal	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H2228	IC₅₀	1.62 μM Compound: Pal	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.22 μM Compound: Pal	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.22 μM Compound: Pal	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay	[PMID: 36628851]
NCI-H3122	IC₅₀	0.26 μM Compound: Pal	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth pretreated with GSH followed by compound addition and incubated for 3 to 5 days by MTT assay	[PMID: 36628851]
OVCAR-3	IC₅₀	>3 μM Compound: 1	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay	[PMID: 34110834]
PC-3	GI₅₀	0.071 μM Compound: Palbociclib	Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay	[PMID: 28156111]
PC-3	IC₅₀	2.2 μM Compound: V	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
Raji	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
RPMI-8226	GI₅₀	2.215 μM Compound: Palbociclib	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]
Sf9	IC₅₀	>10 μM Compound: Palbociclib	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	>10 μM Compound: Palbociclib	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]
Sf9	IC₅₀	>10 μM Compound: Palbociclib	Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	>100 μM Compound: Palbociclib	Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as	[PMID: 30665142]
Sf9	IC₅₀	>100 μM Compound: Palbociclib	Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	0.005 μM Compound: Palbociclib	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	0.013 μM Compound: Palbociclib	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	0.013 μM Compound: Palbociclib	Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay	[PMID: 30665142]
Sf9	IC₅₀	1.1 μM Compound: Palbociclib	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	1.207 μM Compound: Palbociclib	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	8.75 μM Compound: Palbociclib	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	9.1 μM Compound: Palbociclib	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	9.2 μM Compound: PD-0332991	Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP	[PMID: 26851505]
Sf9	IC₅₀	9.8 μM Compound: Palbociclib	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]
SK-MEL19	GI₅₀	30 μM Compound: Palbociclib	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T47D	EC₅₀	0.35 μM Compound: Palbociclib	Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay	[PMID: 30665142]
T47D	GI₅₀	1.056 μM Compound: Palbociclib	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]
U-266	GI₅₀	11.274 μM Compound: Palbociclib	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	IC₅₀	345.2 nM Compound: Palbociclib	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-937	IC₅₀	0.14 μM Compound: Palbociclib	Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis	[PMID: 24641103]
ZR-75-1	GI₅₀	2.279 μM Compound: Palbociclib	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]

In Vitro

Palbociclib (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser⁷⁹⁵ in MDA-MB-435 cells with an IC₅₀ value of 0.063 μM, and obtains similar effects on both Ser⁷⁸⁰ and Ser⁷⁹⁵ phosphorylation in the Colo-205 colon carcinoma^[1].
Palbociclib (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase^[1].
Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells^[2].
Palbociclib (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC₅₀ values ranging from 4 nM to 1 μM^[3].
Palbociclib (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC₅₀ values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest^[4].

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

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-453 cells
Concentration:	0-1 μM
Incubation Time:	24 h
Result:	Arrested MDA-MB-453 cells in G1.

Cell Proliferation Assay^[3]

Cell Line:	ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
Concentration:	0-1 μM
Incubation Time:	6 days
Result:	Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

In Vivo

Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth^[1].
Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects^[2].
Palbociclib (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer^[4].

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

Animal Model:	Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)^[1]
Dosage:	75, 150 mg/kg, daily for 14 days
Administration:	Oral adminstration
Result:	Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.

Animal Model:	Tumor-free female FVB mice^[2]
Dosage:	90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
Administration:	Oral adminstration
Result:	Reduced total thymic mass and immature CD4⁺ and CD8⁺ double-positive thymocytes, and increased the fractions of CD4⁺ and CD8⁺ single-positive thymocytes.

Animal Model:	Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)^[4]
Dosage:	100 mg/kg, daily for 1 week.
Administration:	Oral adminstration
Result:	Decreased the luminescence signal in liver and delayed tumour growth.

Essai clinique

Masse moléculaire

447.53

Formule

C₂₄H₂₉N₇O₂

CAS No.

571190-30-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

0.1 M HCl : 25 mg/mL (55.86 mM; ultrasonic and warming and heat to 60°C)

DMSO : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 5 with HCl; 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	2.2345 mL	11.1724 mL	22.3449 mL
5 mM	0.4469 mL	2.2345 mL	4.4690 mL
10 mM	0.2234 mL	1.1172 mL	2.2345 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, 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.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

Pureté et documentation

Purity: 99.94%

Fiche technique (280 KB) SDS (623 KB)

COA (248 KB) HNMR (206 KB) RP-HPLC (184 KB) MS (69 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Content Brief]

[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [Content Brief]

[3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. [Content Brief]

[4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. [Content Brief]

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