- 英文名称
- (1α,5α,6α)-N-[(2R,14S,18S)-2-[5-(4-Cyclopropyl-1-piperazinyl)-2-[(1S)-1-methoxyethyl]-3-pyridinyl]-1-ethyl-18,19,20,21-tetrahydro-25,25-dimethyl-15,22-dioxo-17H-5,3-([4,2]-endo-thiazolopropano[1,3]-endo-pyridazinomethanoxypropano)-1H-indol-14-yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide
- 分子式
- C47H60N8O6S
- 分子量
- 865.09
- 中文别名
- (1Α,5Α,6Α)-N-[(2R,14S,18S)-2-[5-(4-环丙基-1-哌嗪基)-2-[(1S)-1-甲氧基乙基]-3-吡啶基]-1-乙基-18,19,20,21-四氢-25,25-二甲基-15,22-二氧代-17H-5,3-([4,2]-ENDO-噻唑丙基[1,3]-ENDO-哒嗪甲桥丙烷)-1H-吲哚-14-基]-3-氧杂双环[3.1.0]己烷-6-甲酰胺;化合物 RMC-7977; RMC-7977;(1α,5α,6α)-N-[(2R,14S,18S)-2-[5-(4-Cyclopropyl-1-piperazinyl)-2-[(1S)-1-methoxyethyl]-3-pyridinyl]-1-ethyl-18,19,20,21-tetrahydro-25,25-dimethyl-15,22-dioxo-17H-5,3-([4,2]-endo-thiazolopropano[1,3]-endo-pyridazinomethanoxypropano)-1H-indol-14-yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide;3-Oxabicyclo[3.1.0]hexane-6-carboxamide, N-[(2R,14S,18S)-2-[5-(4-cyclopropyl-1-piperazinyl)-2-[(1S)-1-methoxyethyl]-3-pyridinyl]-1-ethyl-18,19,20,21-tetrahydro-25,25-dimethyl-15,22-dioxo-17H-5,3-([4,2]-endo-thiazolopropano[1,3]-endo-pyridazinomethanoxypropano)-1H-indol-14-yl]-, (1α,5α,6α)-;(3R,4r,5S)-N-((63S,4S,Z)-12-(5-(4-cyclopropylpiperazin-1-yl)-2-((S)-1-methoxyethyl)pyridin-3-yl)-11-ethyl-10,10-dimethyl-5,7-dioxo-61,62,63,64,65,66-hexahydro-11H-8-oxa-2(4,2)-thiazola-1(5,3)-indola-6(1,3)-pyridazinacycloundecaphane-4-yl)tetrahydro-2H-pyran-4-carboxamide
- 用途
- 泛KRAS抑制剂，具有口服活性的三复合RAS抑制剂，可同时结合亲环蛋白A(CYPA)(Kd=195nM)和KRAS(G12V)(Kd=292μM)，对KRAS、NRAS和HRAS三种RAS蛋白及其各种野生型和突变型变体具有广谱抑制活性；通过抑制ERK、CRAF和RSK磷酸化以及增加PARP剪切来诱导细胞凋亡(Apoptosis)，可导致肿瘤消退，减少KRASG12C癌症模型的耐药性，并且在多种RAS癌症模型中具有良好的耐受性。
