- 英文名称
- Rapalink-1
- 分子式
- C91H138N12O24
- 分子量
- 1784.14
- 中文别名
- 42-O-[2-[[1-[32-[4-氨基-3-(2-氨基-5-苯并恶唑基)-1H-吡唑并[3,4-d]嘧啶-1-基]-27-氧代-3,6,9,12,15,18,21,24-八氧杂-28-氮杂三十烷-1-基]-1H-1,2,3-三唑-4-基]甲氧基]乙基]雷帕霉素; 42-O-[2-[[1-[32-[4-氨基-3-(2-氨基-5-苯并噁唑基)-1H-吡唑并[3,4-d]嘧啶-1-基]-27-氧代-3,6,9,12,15,18,21,24-八氧杂-28-氮杂三十烷-1-基]-1H-1,2,3-三唑-4-基]甲氧基]乙基]雷帕霉素; N-(4-(4-氨基-3-(2-氨基苯并[d]恶唑-5-基)-1H-吡唑并[3,4-d]嘧啶-1-基)丁基)-1-(4-((2-(((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-epoxypyrido[2,1-c][1]oxa[4]氮杂环三十一烷-3-基)丙基)-2-甲氧基环己基)氧基)乙氧基)甲基)-1H-1,2,3-三唑-1-基)-3,6,9,12,15,18,21,24-八氧杂二十七烷-27-酰胺; RAPALINK 1; RAPALINK1; SCHEMBL19294565; N-[4-[4-amino-3-(2-amino-1,3-benzoxazol-5-yl)pyrazolo[3,4-d]pyrimidin-1-yl]butyl]-3-[2-[2-[2-[2-[2-[2-[2-[2-[4-[2-[(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl]oxyethoxymethyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanamide; 42-O-[2-[[1-[32-[4-Amino-3-(2-amino-5-benzoxazolyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-27-oxo-3,6,9,12,15,18,21,24-octaoxa-28-azadotriacont-1-yl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]rapamycin; N-(4-(4-Amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)butyl)-1-(4-((2-(((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)oxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-amide
- 用途
- RapaLink-1 是第三代 mTOR 抑制剂,通过 linker 将雷帕霉素与二代 mTOR 抑制剂 MLN0128 结合,比雷帕霉素或 mTOR 抑制剂更有效,能有效阻断癌源性的、激活的 mTOR 突变体,可穿过血脑屏障,与 FKBP12 结合导致持久抑制 mTORC1,通过促进自噬在抗磷脂综合征中发挥抗血栓作用,具有抗癌活性,用于化学合成。