Size | Price | Stock |
---|---|---|
2mg | $130 | In-stock |
5mg | $230 | In-stock |
10mg | $320 | In-stock |
50mg | $950 | In-stock |
100 mg | Get quote | |
200 mg | Get quote | |
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Cat. No. : | HY-100888 |
M.Wt: | 341.43 |
Formula: | C17H19N5OS |
Purity: | >98 % |
Solubility: | DMSO : 75 mg/mL (219.66 mM; Need ultrasonic) |
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity[1]. IC50 & Target: IC50: <0.3 nM (CDC7 kinase)[1]. 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[1]. 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[1].
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