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Simurosertib (TAK-931)

  Cat. No.:  DC21653   Featured
Chemical Structure
1330782-76-7
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Field of application
TAK-931 (Simurosertib) is a potent, selective, ATP competitive and orally bioavailable inhibitor of Cdc7 with IC50 of <0.3 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1330782-76-7
Chemical Name: Simurosertib
Synonyms: Simurosertib;Tak 931;LST350G3XU;Thieno(3,2-d)pyrimidin-4(3H)-one, 2-(2S)-1-azabicyclo(2.2.2)oct-2-yl-6-(3-methyl-1H-pyrazol-4-yl)-;TAK931;2-[(2S)-1-azabicyclo[2.2.2]octan-2-yl]-6-(5-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one;2-((2S)-1-azabicyclo(2.2.2)octan-2-yl)-6-(5-methyl-1H-pyrazol-4-yl)-3H-thieno(3,2-d)pyrimidin-4-one;2-[(2S)-1-azabicyclo[2.2.2]octan-2-yl]-6-(5-methyl-1H-pyrazol-4-yl)-3H-thieno[3,2-d]pyrimidin-4-one;TAK-931
SMILES: S1C(C2C=NNC=2C)=CC2=C1C(NC([C@@H]1CC3CCN1CC3)=N2)=O
Formula: C17H19N5Os
M.Wt: 341.430661439896
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: TAK-931 is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM.
Target: IC50: <0.3 nM (CDC7 kinase)[1].
In Vivo: In the COLO205-xenograft mouse model, oral administration of TAK-931 inhibits pMCM2 of the xenografted COLO205 in dose- and time-dependent manners. Furthermore, TAK-931 exhibits a significant antitumor activity in multiple xenograft models[1].
In Vitro: 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 TAK-931 for CDC7 kinase inhibition compared to other kinase inhibitions. Treatment with 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].
References: [1]. K Iwai, et al. A novel CDC7-selective inhibitor TAK-931 with potent antitumor activity. European Journal of Cancer , 2016 , 69 (1) :S34.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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