Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).
説明 | Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM). |
ターゲット&IC50 | CDC7:<0.3 nM |
In vitro | 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]. |
In vivo | 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]. |
別名 | TAK-931 |
分子量 | 341.43 |
分子式 | C17H19N5OS |
CAS No. | 1330782-76-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 75 mg/mL (219.66 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Simurosertib 1330782-76-7 Cell Cycle/Checkpoint CDK Inhibitor anti-cancer TAK-931 Cyclin dependent kinase ATP-competitive TAK931 cycle cell orally inhibit TAK 931 division inhibitor