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Simurosertib
Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).
Catalog No. T12642LCas No. 1330782-76-7
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Simurosertib
Catalog No. T12642LAlias TAK-931Cas No. 1330782-76-7
Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $68 | In Stock | |
| 2 mg | $97 | In Stock | |
| 5 mg | $189 | In Stock | |
| 10 mg | $263 | In Stock | |
| 25 mg | $489 | In Stock | |
| 50 mg | $713 | In Stock | |
| 100 mg | $987 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $196 | In Stock |
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CitedProduct Introduction
Bioactivity
Chemical Properties
| Description | Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM). |
| Targets&IC50 | CDC7:<0.3 nM |
| In vitro | Simurosertib effectively inhibits CDC7 kinase activity (IC50 <0.3 nM) with time-dependent ATP-competitive kinetics to its ATP-binding pocket. Treatment with Simurosertib inhibits the cellular MCM2 phosphorylation at Ser40 in a dose-dependent manner, resulting in a delayed S phase progression, DNA-damage checkpoint activation, and caspase-3/7 activation. The selectivity studies using the 308 kinases reveals >120-fold selectivity of Simurosertib for CDC7 kinase inhibition compared to other kinase inhibitions [1]. |
| In vivo | Simurosertib (p.o.) inhibits pMCM2 of the xenografted COLO205 in a dose- and time-dependent manner in the COLO205-xenograft mouse model. Simurosertib shows a significant antitumor activity in multiple xenograft models [1]. |
| Alias | TAK-931 |
| Molecular Weight | 341.43 |
| Formula | C17H19N5OS |
| Cas No. | 1330782-76-7 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (131.8 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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