S49076 HCl 是 MET、AXL/MER 和 FGFR1/2/3 的有效抑制剂。 S49076 在体外和体内有效阻断 MET、AXL 和 FGFR 的细胞磷酸化并抑制下游信号传导。在细胞模型中，S49076 抑制 MET 和 FGFR2 依赖性胃癌细胞的增殖，阻断 MET 驱动的肺癌细胞迁移，并抑制表达 FGFR1/2 和 AXL 的肝癌细胞的集落形成。在肿瘤异种移植模型中，建立了口服 S49076 后 MET 和 FGFR2 抑制的良好药代动力学/药效学关系，并与对肿瘤生长的影响密切相关。

S49076 is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 was established and correlated well with impact on tumor growth.

1265966-31-1

C22H23ClN4O4S

474.96

S-49076 Hydrochloride

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years