Simurosertib(TAK-931)是CDC7激酶的选择性抑制剂，其IC50值<0.3nM。
CAS：1330782-76-7
分子式：C17H19N5OS
分子量：341.43
纯度：98%
存储：Store at -20°C

Background:

Simurosertib (TAK-931) is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM.

Simurosertib (TAK-931) potently inhibits CDC7 kinase activity (IC50 120-fold selectivity of Simurosertib (TAK-931) for CDC7 kinase inhibition compared to other kinase inhibitions. Treatment with Simurosertib (TAK-931) suppresses the cellular MCM2 phosphorylation at Ser40 (pMCM2) in a dose-dependent manner, resulting in a delayed S phase progression, DNA-damage checkpoint activation, and caspase-3/7 activation[1].

In the COLO205-xenograft mouse model, oral administration of Simurosertib (TAK-931) inhibits pMCM2 of the xenografted COLO205 in dose- and time-dependent manners. Furthermore, Simurosertib (TAK-931) exhibits a significant antitumor activity in multiple xenograft models[1].

[1]. K Iwai, et al. A novel CDC7-selective inhibitor TAK-931 with potent antitumor activity. European Journal of Cancer , 2016 , 69 (1) :S34.