| CAS NO: | 1330782-76-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Name: Simurosertib / TAK-931 CAS#: 1330782-76-7 Chemical Formula: C17H19N5OS Exact Mass: 341.131 Molecular Weight: 341.433 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: TAK931; TAK 931; TAK-931; Simurosertib Chemical Name: 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)- InChi Key: XGVXKJKTISMIOW-ZDUSSCGKSA-N InChi Code: InChI=1S/C17H19N5OS/c1-9-11(8-18-21-9)14-7-12-15(24-14)17(23)20-16(19-12)13-6-10-2-4-22(13)5-3-10/h7-8,10,13H,2-6H2,1H3,(H,18,21)(H,19,20,23)/t13-/m0/s1 SMILES Code: O=C1C2=C(C=C(C3=CNN=C3C)S2)N=C([C@H]4N(CC5)CCC5C4)N1 |
| Target | IC50:<0.3 nM (CDC7 kinase)[1]. |
|---|---|
| In Vitro | TAK-931 potently inhibits CDC7 kinase activity (IC50<0.3 308="" with="" a="" time-dependent="" atp-competitive="" kinetics="" to="" its="" atp-binding="" pocket.="" the="" selectivity="" studies="" using="" 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]. |
| 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]. |
| References | [1]. A novel CDC7-selective inhibitor TAK-931 with potent antitumor activity. European Journal of Cancer , 2016 , 69 (1) :S34. |
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