AZD3229 _c-Kit 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAZD3229Cat. No.: HY-112802CAS No.: 2248003-60-1分式: CHFNO分量: 479.51作靶点: c-Kit作通路: Protein Tyrosine Kinase/RTK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 : 100 mg/mL (208.55 mM)* means solu

2、ble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0855 mL 10.4273 mL 20.8546 mL5 mM 0.4171 mL 2.0855 mL 4.1709 mL10 mM 0.2085 mL 1.0427 mL 2.0855 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。BIOLOGICAL ACTIVITY物活性 AZD3229种有效的、泛的突变型酪氨酸激酶受体 (KIT) 抑制剂，可于开发治疗胃肠道间质瘤。IC50 &

3、 Target KIT 1.体外研究AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diversepanel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM). AZD3229 demonstrates potent single digit nM1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEgrowth inhibition acr

4、oss a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR canbe rationalised predominantly by the interaction of water molecules with the protein and ligand in the activesite and its kinome selectivity is similar to the best of the approved GIST agents 1.REFERENCES1. Kettl

5、e JG, et al. Discovery of N-(4-5-Fluoro-7-(2-methoxyethoxy) quinazolin-4-ylamino phenyl)-2-4-(propan-2-yl)-1 H-1,2,3-triazol-1-ylacetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct11;61(19):8797-8810.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-