RET-IN-4

Name: RET-IN-4
Brand: TargetMol
SKU: T40097
Rating: 4.5 (1 reviews)

还可以

产品编号 T40097Cas号 2436473-55-9

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.

RET-IN-4

还可以

产品编号 T40097Cas号 2436473-55-9

规格	价格	库存	数量
25 mg	¥ 10,600	6-8周

大包装 & 定制

加入购物车

TargetMol 的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

联系我们获取更多批次信息

资源下载

产品操作手册

产品介绍

生物活性

产品描述	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.
靶点活性	RET (WT):1.29 nM (IC50), RET (M918T):0.99 nM (IC50), RET (V804M):1.97 nM (IC50)
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.