RET-IN-4 T40097

Product Introduction
Bioactivity


英文名: RET-IN-4

描述: RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties.

体外活性: The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC 50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667[1].

体内活性: RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner[1]. Animal Model: Immunodeficient nude/nude mice bearing KIF5B-RET Ba/F3 cells[1]Dosage: 10 mg/kg, 20 mg/kg Administration: p.o.; daily; for 10 days Result: The tumor growth was remarkably suppressed.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: RET-IN-4 | RETIN4 | RET IN 4

RET-IN-4 T40097信息由TargetMol中国为您提供，如您想了解更多关于RET-IN-4 T40097报价、型号、参数等信息，欢迎来电或留言咨询。

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