571189-11-2

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

DYRK1A: 2000 nM (IC₅₀); MAPK: 8000 nM (IC₅₀); Cdk4/cyclin D3: 9 nM (IC₅₀); Cdk4/cyclin D1: 11 nM (IC₅₀); Cdk6/cyclin D2: 16 nM (IC₅₀)

[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. PMID:15542782
[2] Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. DOI:10.1038/nature23465
[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. DOI:10.1186/bcr2419
[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. DOI:10.1136/gutjnl-2016-312268