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S49076 是一种新型 MET、AXL/MER 和 FGFR1/2/3 高效抑制剂,IC50<20 nM。
S49076 是一种新型 MET、AXL/MER 和 FGFR1/2/3 高效抑制剂,IC50<20 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 289 | 现货 | |
2 mg | ¥ 413 | 现货 | |
5 mg | ¥ 578 | 现货 | |
10 mg | ¥ 913 | 现货 | |
25 mg | ¥ 1,690 | 现货 | |
50 mg | ¥ 2,890 | 现货 | |
100 mg | ¥ 4,780 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs. |
靶点活性 | Axl:7 nM, Mer:2 nM, FGFR3:15 nM, MET:1 nM, FGFR2:17 nM |
体外活性 | S49076 強效地阻斷 MET、AXL 和 FGFRs 的细胞磷酸化,并在体外和体内抑制下游信号传导。在细胞模型中,S49076 抑制依赖 MET 和 FGFR2 的胃癌细胞增殖,阻止 MET 驱动的肺癌细胞迁移,以及抑制表达 FGFR1/2 和 AXL 的肝癌细胞的集落形成。S49076 对表达 MET、AXL 或 FGFRs 的癌细胞的活性、移动性和三维集落形成均有抑制作用[1]。 |
体内活性 | S49076在经受MET和FGFR依赖的肿瘤异种移植物中展示出显著的抗肿瘤活性,并且在被良好容忍的剂量下效果显著。该化合物对肿瘤的分布高,其中3.125 mg/kg剂量的半衰期约为7小时,相比之下血液中的半衰期不足2小时。在6.25 mg/kg及以上剂量时,MET磷酸化抑制率在16小时后保持超过50%。S49076还在贝伐珠单抗抵抗模型中显示活性,并且与贝伐珠单抗联用完全抑制结肠癌异种移植物的生长[1]。 |
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) |
分子量 | 438.5 |
分子式 | C22H22N4O4S |
CAS No. | 1265965-22-7 |
Smiles | O=C1CSC(=O)N1Cc1ccc2NC(=O)\C(=C/c3cc(CN4CCOCC4)c[nH]3)c2c1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 81 mg/mL (184.9 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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