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Simurosertib
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图片
CAS NO:1330782-76-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
TAK-931
产品介绍
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。

产品描述

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

体外活性

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].

体内活性

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].

Cas No.

1330782-76-7

分子式

C17H19N5OS

分子量

341.43

别名

TAK-931

储存和溶解度

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