AZD3229 _c-Kit 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAZD3229Cat. No.: HY-112802CAS No.: 2248003-60-1分式: CHFNO分量: 479.51作靶點: c-Kit作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (208.55 mM)* means solu

2、ble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 AZD3229種有效的、泛的突變型酪氨酸激酶受體 (KIT) 抑制劑，可于開發(fā)治療胃腸道間質(zhì)瘤。IC50 &

3、 Target KIT 1.體外研究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 您邊的抑制劑師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-