Savolitinib 是一种高效选择性、口服生物利用度c-Met抑制剂,能够抑制 c-Met (IC50:5 nM)和 p-Met (IC50:3 nM)。它以 ATP 竞争的方式选择性结合并抑制 c-Met 的激活,破坏 c-Met 信号转导途径,具有抗肿瘤作用。
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Savolitinib (AZD-6094) is an effective, selective, and orally bioavailable c-Met inhibitor (IC50s: 5 nM/3 nM for c-Met/p-Met).
体外活性
Savolitinib selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways [1,2].
体内活性
In a U87MG subcutaneous xenograft model, Savolitinib (1-10.0 mg/kg; oral administration; daily; for 21 days; athymic nude mice) demonstrates dose-dependent tumor growth inhibition. In addition, none of the mice in the dosing groups exhibits body weight loss during the experiment [1].
Cas No.
1313725-88-0
分子式
C17H15N9
分子量
345.36
别名
AZD-6094;沃利替尼;HMPL-504;赛沃替尼;Volitinib
储存和溶解度
DMSO:32 mg/mL (92.65 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years