Simurosertib - 半岛电竞官方网址

	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

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.

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.

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