- 英文名称
- Deforolimus
- 分子式
- C53H84NO14P
- 分子量
- 990.21
- 中文别名
- 雷帕霉素衍生物; MTOR抑制剂(DEFOROLIMUS); (二甲基亚膦酰)雷帕霉素; RIDAFOROLIMUS DEFOROLIMUS; (1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-二羟基-10,21-二甲氧基-6,8,12,14,20,26-六甲基-1,5,11,28,29-五氧代-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-二十四氢-3H-23,27-环氧吡啶并[2,1-c][1]氮杂环三十一烷-3-基)丙基)-2-甲氧基环己基 二甲基亚膦酸酯; 42-(Dimethylphosphinate)rapamycin; Ridaforolimus; (1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-Dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl dimethylphosphinate
- 用途
- Ridaforolimus (Deforolimus, MK-8669)是一种选择性的mTOR抑制剂,IC50为0.2 nM;对mTOR信号通路的抑制作用及与FKBP12结合能力和Rapamycin接近。体外研究显示其能抑制S6和4E-BP1磷酸化,具有剂量依赖性,导致细胞尺寸降低,G1期细胞增多,抑制葡萄糖摄取,有效且选择性抑制VEGF产量。体内研究表明其处理携带多种移植瘤的小鼠具有显著抗癌效果,抑制mTOR信号。