- 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
- 9001421-10
- 产品报价
- ￥1/50mg
- 产品说明书
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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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