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Simurosertib(TAK-931)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Simurosertib(TAK-931)图片
CAS NO:1330782-76-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
Simurosertib (TAK-931) (TAK-931) 是一种具有口服活性、选择性和 ATP 竞争性细胞分裂周期 7 (CDC7) 激酶抑制剂，IC50<0.3 nM。 Simurosertib (TAK-931) 具有抗癌活性。
Cas No.1330782-76-7
别名TAK-931
Canonical SMILESO=C1C2=C(C=C(C3=CNN=C3C)S2)NC([C@H]4N(CC5)CCC5C4)=N1
分子式C17H19N5OS
分子量341.43
溶解度DMSO : 75 mg/mL (219.66 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.