1. Cell Cycle/DNA Damage
  2. CDK

Simurosertib (Synonyms: TAK-931)

Cat. No.: HY-100888 Purity: 99.04% ee.: 99.91%
Handling Instructions

Simurosertib (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.

Simurosertib Chemical Structure

Simurosertib Chemical Structure

CAS No. : 1330782-76-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 244 In-stock
Estimated Time of Arrival: December 31
2 mg USD 130 In-stock
Estimated Time of Arrival: December 31
5 mg USD 230 In-stock
Estimated Time of Arrival: December 31
10 mg USD 320 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 Get quote
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200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

Cdc7

0.3 nM (IC50)

In Vitro

Simurosertib (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 Simurosertib (TAK-931) for CDC7 kinase inhibition compared to other kinase inhibitions. Treatment with Simurosertib (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 Simurosertib (TAK-931) inhibits pMCM2 of the xenografted COLO205 in dose- and time-dependent manners. Furthermore, Simurosertib (TAK-931) exhibits a significant antitumor activity in multiple xenograft models[1].

Clinical Trial
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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Simurosertib
Cat. No.:
HY-100888
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Simurosertib

Cat. No.: HY-100888