| Description |
TAK-931 is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM.
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| Related Catalog |
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| Target |
IC50: <0.3 nM (CDC7 kinase)[1].
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| 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].
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| 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].
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| 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.
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