Simurosertib


CAS No. : 1330782-76-7

(Synonyms: TAK-931)

1330782-76-7
Price and Availability of CAS No. : 1330782-76-7
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2mg $130 In-stock
5mg $230 In-stock
10mg $320 In-stock
50mg $950 In-stock
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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)
Introduction of 1330782-76-7 :

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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