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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
TAK-931
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1330782-76-7
- 规格：
10 mM * 1 mL/2 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2817.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥1463.0 |
| 规格： | 5 mg | 产品价格： | ￥2300.0 |
| 规格： | 10 mg | 产品价格： | ￥3663.0 |
| 规格： | 25 mg | 产品价格： | ￥5860.0 |
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Simurosertib
CAS No. : 1330782-76-7
MCE 国际站：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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