Simurosertib 是一种选择性和 ATP 竞争性细胞分裂周期 7 激酶抑制剂，具有抗癌活性，IC50值小于 0.3 nM。

Simurosertib is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50:<0.3 nM).

Simurosertib effectively inhibits CDC7 kinase activity (IC50<0.3 nM) with time-dependent ATP-competitive kinetics to its ATP-binding pocket. Treatment with Simurosertib inhibits the cellular MCM2 phosphorylation at Ser40 in a dose-dependent manner, resulting in a delayed S phase progression, DNA-damage checkpoint activation, and caspase-3/7 activation. The selectivity studies using the 308 kinases reveals >120-fold selectivity of Simurosertib for CDC7 kinase inhibition compared to other kinase inhibitions [1].

Simurosertib (p.o.) inhibits pMCM2 of the xenografted COLO205 in a dose- and time-dependent manner in the COLO205-xenograft mouse model. Simurosertib shows a significant antitumor activity in multiple xenograft models [1].

1330782-76-7

C17H19N5OS

341.43

TAK-931

DMSO:75 mg/mL (219.66 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years