化合物S49076 T3274
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 1265965-22-7 | ¥4,780.00 | 询底价 |
1 mg | 1265965-22-7 | ¥289.00 | 询底价 |
50 mg | 1265965-22-7 | ¥2,890.00 | 询底价 |
25 mg | 1265965-22-7 | ¥1,690.00 | 询底价 |
2 mg | 1265965-22-7 | ¥413.00 | 询底价 |
5 mg | 1265965-22-7 | ¥578.00 | 询底价 |
1 mL | 1265965-22-7 | ¥638.00 | 询底价 |
10 mg | 1265965-22-7 | ¥913.00 | 询底价 |
Product Introduction
Bioactivity
英文名: S49076
描述: S49076 是一种新型 MET、AXL/MER 和 FGFR1/2/3 高效抑制剂,IC50<20 nM。
细胞实验: For GTL-16 and SNU-16 viability assays, cells are seeded in 96-well microplates at the appropriate density in media containing 10% FCS and supplemented 48 hours later with serial dilutions of S49076 in a final volume of 150 μL per well. After 96 hours (GTL-16) or 120 hours (SNU-16) incubation, 15 μL of a solution of 5 mg/mL MTT is added to each well and the plates are incubated for 4 hours at 37℃. The formazan metabolite is solubilized in SDS for SNU-16 and, following removal of the MTT solution, in DMSO for GTL-16. Global cell viability is estimated by measurement of optical density at 540 nm. (Only for Reference)
体外活性: S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling in vitro and in vivo. In cell models, S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. S49076 inhibits viability, motility, and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs[1].
体内活性: S49076 shows marked antitumor activity in MET- and FGFR-dependent tumor xenografts at well-tolerated doses. S49076 has high distribution to tumors, in which the half-life for the dose of 3.125 mg/kg is approximately 7 hours versus less than 2 hours in the blood. At doses of 6.25 mg/kg and higher, more than 50% inhibition of MET phosphorylation is retained at 16 hours. S49076 is also active in a bevacizumab-resistant model and totally inhibits the growth of colon carcinoma xenografts in association with bevacizumab[1].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 81 mg/mL (184.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字: FGFR | Fibroblast growth factor receptor | inhibit | c-Met/HGFR | S49076 | Inhibitor | S 49076 | S-49076
相关产品: FGFR4-IN-1 | Zoligratinib | Dovitinib lactate hydrate | PD-166866 | Gandotinib | BLU9931 | Lenvatinib | Bemarituzumab | FIIN-4 | KHS101 hydrochloride
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Osteogenesis Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途