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Simurosertib

CAS No. : 1330782-76-7

MCE 站：Simurosertib

产品活性：Simurosertib (TAK-931) 是一种具有口服活性，选择性， ATP 竞争性的细胞分裂周期 7 (CDC7) 激酶抑制剂，IC₅₀ 为 <0.3 nM。Simurosertib 具有抗癌活性。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: Simurosertib (TAK-931) potently inhibits CDC7 kinase activity (IC₅₀ <0.3 nM) with a time-dependent ATP-competitive kinetics to its ATP-binding pocket. The selectivity studies using the 308 kinases reveals >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.

In Vivo: 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.

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