Simurosertib-TAK-931-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESimurosertibCat. No.: HY-100888CAS No.: 1330782-76-7Synonyms: TAK-931分式: CHNOS分量: 341.43作靶点: CDK作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 75 mg/mL (219.66 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9289 mL 14.6443 mL 29.2886 mL5 mM 0.5858 mL 2.9289 mL 5.8577 mL10 mM 0.2929 mL 1.4644 mL 2.9289 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可

3、以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.32 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.32 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecu

4、les 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.32 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Simurosertib (TAK-931)是CDC7 激酶的选择性抑制剂，其 IC50 值 0.3 nM。IC50 & Target Cdc70.3 nM (IC50)体外研究 Simurosertib (TAK-931) potently inhibits CDC7 kinase activity (IC50 120-fold selectivity of Simurosertib (TAK-931) fo

5、r 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 ina delayed S phase progression, DNA-damage checkpoint activation, and caspase-3/7 activation 1.体内研究

6、 In the COLO205-xenograft mouse model, oral administration of Simurosertib (TAK-931) inhibits pMCM2 ofthe xenografted COLO205 in dose- and time-dependent manners. Furthermore, Simurosertib (TAK-931)exhibits a significant antitumor activity in multiple xenograft models 1.户使本产品发表的科研献 Breast Cancer Res

7、. 2019 Jul 1;21(1):77.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. K Iwai, et al. A novel CDC7-selective inhibitor TAK-931 with potent antitumor activity. European Journal of Cancer , 2016 , 69 (1) :S34.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use