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P276-00 920113-03-7

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Synonyms
Appearance
Chemical Formula
C21H20ClNO5.HCl
Solubility
Molecular Weight
438.3
Storage and Stability
in stock
CAS No.
920113-03-7
Purity
98%+
Introduction
P276-00 is a novel CDK1CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively.

P276-00 shows 40-fold selectivity toward Cdk4-D1, compared with Cdk2-E. It shows potent antiproliferative effects against various human cancer cell lines, including HCT-116, U2OS, H-460, HL-60, HT-29, SiHa, MCF-7, Colo-205, SW-480, PC-3, Caco2, T-24 with an IC50 ranging from 300 to 800 nmol/L, and is found to be highly selective for cancer cells as compared with normal fibroblast cells. P276-00 can down-regulate cyclin D1 and Cdk4 in an ATP- competitive manner and decrease Cdk4-specific pRb Ser780 phosphorylation. P276-00 also induces apoptosis by actving cellular caspase-3 activity and DNA ladder formation

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