802539-81-7

PHA-848125/PHA848125

802539-81-7

编号ABP000843 化学名称PHA-848125/PHA848125 英文名称 PHA-848125/PHA848125 分子式C25H32N8O 分子量460.5746 纯度 99%

化学名称 : PHA-848125/PHA848125

CAS : 802539-81-7

英文名称: PHA-848125/PHA848125

英文同义词: 4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

溶解度:DMSO

储存条件:at -20C 2 years

生物活性

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.

参考文献

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.

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