BMS-265246

"目录号: HY-15275

Cell Cycle/DNA Damage-

BMS-265246是CDK1/2抑制剂，对CDK1/cyclin B和CDK2/cyclin E的IC50分别为6 nM和9 nM。

CDK

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生物活性

Description

BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively. IC50 Value: 6 nM(for CDK1/cyclin B); 9 nM(for CDK2/cyclin E)Target: CDK1/2in vitro: BMS-265246 inhibits the activity of Cdk4/cycD (IC50 = 0.23 μM) and prevents A2780 Cytox with IC50 of 0.76 μM. BMS-265246 when bound to Cdk2, shows the inhibitor resides within the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone. BMS-265246 represents the most potent Cdk/Cdk2 selective analogue from this chemotype. 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.in vivo:

References

[1].Misra RN, Xiao H, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8.