Chemical Name : PHA-848125/PHA848125
CAS : 802539-81-7
Storage:at -20C 2 years
PD-0332991 is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. This compound is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4) (IC50, 0.011 umol/L) and Cdk6 (IC50, 0.016 umol/L), having no activity against a panel of 36 additional protein kinases.Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and downregulation of genes under the transcriptional control of E2F.This agent shows significant inhibition in a broad spectrum of human tumor xenografts in vivo.
1. Menu E, Garcia J, Huang X, Di Liberto M, Toogood PL, Chen I, Vanderkerken K, Chen-Kiang S. A novel therapeutic combination using PD 0332991 and bortezomib: study in the 5T33MM myeloma model. Cancer Res. 2008 Jul 15;68(14):5519-23.