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BMS-265246 582315-72-8

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Synonyms ：
Appearance ：
Chemical Formula ：
C18H17F2N3O2
Solubility ：
Molecular Weight ：
345.34
Storage and Stability ：
in stock
CAS No. ：
582315-72-8
Purity ：
98%+
Introduction
BMS-265246 is a 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 inhibits the activity of CDK4/cycD with IC50 of 0.23 μM and prevents A2780 Cytox with IC50 of 0.76 μM. BMS265246 which binds to CDK2 shows the inhibitor resides coincident with the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone. BMS265246 exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent versus CDK1 and CDK2, respectively. BMS265246 represents the most potent CDK/CDK2 selective analogue from this chemotype. [1] A recent study shows that BMS-265246 inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of BMS-265246, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity. [2]

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