TAK-931

Names

[ Name ]:
TAK-931

[Synonym ]:
2-[(2S)-1-Azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one
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)-
LST350G3XU
TAK-931
Simurosertib

Biological Activity

[Description]:

TAK-931 is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM.

[Related Catalog]:

Research Areas >> Cancer

[Target]

IC50: <0.3 nM (CDC7 kinase)[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].

[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]. K Iwai, et al. A novel CDC7-selective inhibitor TAK-931 with potent antitumor activity. European Journal of Cancer , 2016 , 69 (1) :S34.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Molecular Formula ]:
C₁₇H₁₉N₅OS

[ Molecular Weight ]:
341.431

[ Exact Mass ]:
341.131042

[ LogP ]:
1.76

[ Index of Refraction ]:
1.870

Related Compounds

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