1. Cell Cycle/DNA Damage
  2. CDK

TAK-931 

Cat. No.: HY-100888
Handling Instructions

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

For research use only. We do not sell to patients.

TAK-931 Chemical Structure

TAK-931 Chemical Structure

CAS No. : 1330782-76-7

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9289 mL 14.6443 mL 29.2886 mL
5 mM 0.5858 mL 2.9289 mL 5.8577 mL
10 mM 0.2929 mL 1.4644 mL 2.9289 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

341.43

Formula

C₁₇H₁₉N₅OS

CAS No.

1330782-76-7

SMILES

O=C1C2=C(C=C(C3=CNN=C3C)S2)NC([[email protected]]4N(CC5)CCC5C4)=N1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TAK-931
Cat. No.:
HY-100888
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TAK-931

Cat. No.: HY-100888