PD0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) (~0.011 µM) and Cdk6 (~0.016 µM), having no activity against a panel of 36 additional protein kinases. PD0332991 causes elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and downregulation of genes under the transcriptional control of E2F. It has showed significant inhibition in a broad spectrum of human tumor xenografts in vivo.
Technical information:
Chemical Formula: | C24H29N7O2 | |
CAS #: | 571190-30-2 | |
Molecular Weight: | 447.53 | |
Purity: | >98% | |
Appearance: | White solid | |
Chemical Name: | 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | |
Solubility: | Up to 100 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
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;3(11):1427-38 |
2. | Eline Menu, et al. A Novel Therapeutic Combination Using PD 0332991 and Bortezomib: Study in the 5T33MM Myeloma Model. Cancer Res 2008;68:5519-5523 |
3. | Finn RS, 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. |
Other Information:
Product Specification (pdf)
MSDS (pdf)