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Description: BMS-265246 is a novel, potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4. BMS265246 inhibited the Cdk4/cycD activity and prevented A2780 Cytox (IC50 = 0.23 uM and 0.76 uM). In HCT-116 cells, BMS-265246 blocked the cell proliferation (EC50= 0.293 um—0.492 um). Following the treatment of BMS-265246, low DNA intensity, large round nuclei and 4N DNA content were observed in the dominant cell population –G2 arrested cells.
References: Bioorg Med Chem Lett. 2003 Jul 21; 13(14):2405-8; Mol Cancer Ther. 2011 Feb; 10(2):242-54.
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