中文名称

1-（4-（4-氨基-1-异丙基-1H-吡唑并[3,4-d]嘧啶-3-基）苯基）-3-（2-氟-5-（三氟甲基）苯基）脲，一盐酸盐

英文名字

1-(4-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)phenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea, monohydrochloride

供应商

开曼生物

产品货号

9001421-1

产品报价

￥1/50mg

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产品新闻

背景资料

Multiple endocrine neoplasia type 2B (MEN2B) typically involves an autosomal-dominant activating germline mutation in the gene for Ret (rearranged during transfection), a receptor tyrosine kinase.{25682} Mutation in Ret, denoted as dRetMEN2B, results in medullary thyroid carcinoma, as well as other pathological abnormalities.{25682} AD80 is a potent inhibitor of dRetMEN2B (IC50 = 4 nM), as well as downstream kinases, including Raf, Src, and S6 kinase.{21665} Importantly, AD80 does not inhibit mTOR (IC50 > 10 ?M), which allows mTOR to maintain its normal function of inhibiting signaling through Raf.{21665} Through these combined actions, AD80 displays high efficacy against multiple endocrine neoplasia type 2B (MEN2B) cancer cells without cytotoxicity against other cell types.{21665} In nude mice, AD80 promotes tumor growth inhibition of MEN2B xenografts without significant weight loss.{21665}

产品描述

A potent inhibitor of dRetMEN2B (IC50 = 4 nM), as well as downstream kinases, including Raf, Src, and S6 kinase; does not inhibit mTOR (IC50 > 10 ?M), which allows mTOR to maintain its normal function of inhibiting signaling through Raf; displays high efficacy against MEN2B cancer cells without cytotoxicity against other cell types

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