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Palbociclib is an orally bioavailable selective inhibitor of CDK4 and CDK6, kinases that regulate cell cycle progression. This compound exhibits anticancer chemotherapeutic activity in a variety of models, including renal cell carcinoma and ER+ breast cancer. Palbociclib inhibits retinoblastoma phosphorylation, preventing cells from progressing from the G1 phase to the S phase and inducing apoptosis.
| Cas No. | 827022-32-2 |
|---|---|
| Purity | ≥99% |
| Formula | C24H29N7O2 • HCl |
| Formula Wt. | 483.99 |
| IUPAC Name | 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;hydrochloride |
| Synonym | PD-0332991 |
| Solubility | Soluble in DMSO and water |
| Appearance | Yellow Powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet |
Logan JE, Mostofizadeh N, Desai AJ, et al. PD-0332991, a Potent and Selective Inhibitor of Cyclin-dependent Kinase 4/6, Demonstrates Inhibition of Proliferation in Renal Cell Carcinoma at Nanomolar Concentrations and Molecular Markers Predict for Sensitivity. Anticancer Res. 2013 Aug;33(8):2997-3004. PMID: 23898052.
Roberts PJ, Bisi JE, Strum JC, et al. Multiple roles of cyclin-dependent kinase 4/6 inhibitors in cancer therapy. J Natl Cancer Inst. 2012 Mar 21;104(6):476-87. PMID: 22302033.
Rivadeneira DB, Mayhew CN, Thangavel C, et al. Proliferative suppression by CDK4/6 inhibition: complex function of the retinoblastoma pathway in liver tissue and hepatoma cells. Gastroenterology. 2010 May;138(5):1920-30. PMID: 20100483.
