NU6140是一种选择性的CDK2-cyclinA抑制剂(IC50，0.41μM)，对其选择性是对其他CDK的10-36倍。NU6140有效抑制AuroraA和AuroraB的活性，IC50值分别为67和35nM。抗肿瘤作用。
CAS：444723-13-1
分子式：C23H30N6O2
分子量：422.52
纯度：98%
存储：Store at -20°C

Background:

NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs[1]. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively[2]. Anti-cancer activity[1][2]. cdk2-cyclin A|0.41 μM (IC50)|CDK1-Cyclin B|6.6 μM (IC50)|CDK4-Cyclin D|5.5 μM (IC50)|cdk5-p25|15 μM (IC50)|cdk7-cyclin H|3.9 μM (IC50)|Aurora A|67 nM (IC50)|Aurora B|35 nM (IC50)

NU6140 is less active on CDK1-cyclin B, CDK4-cyclin D, CDK5-p25 and CDK7-cyclin H, with IC50s of 0.41, 6.6, 5.5, 15 and 3.9 μM, respectively[1].NU6140 increases catalytic activity of capase-9 and capase-3, causes increase in the sub-G1 apoptotic cell population[1].

[1]. Pennati M, et al. Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37.