| Name | Simurosertib |
| Description | Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.86 mM), Sonication is recommended.
DMSO : 47 mg/mL (137.66 mM), Sonication is recommended.
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| Keywords | TAK931 | TAK 931 | Simurosertib | orally | Inhibitor | inhibit | division | Cyclin dependent kinase | cycle | cell | CDK | Cdc7 | ATP-competitive | anti-cancer |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
