- 英文名称
- Seletalisib
- 分子式
- C23H14ClF3N6O
- 分子量
- 482.85
- 中文别名
- 塞来利司; 塞来利西布; (R)-3-(8-氯-3-(2,2,2-三氟-1-(吡啶并[3,2-d]嘧啶-4-基氨基)乙基)喹啉-2-基)吡啶 1-氧化物; UCB5857; UCB-5857; UCB 5857; N-{(1R)-1-[8-Chloro-2-(1-oxido-3-pyridinyl)-3-quinolinyl]-2,2,2-trifluoroethyl}pyrido[3,2-d]pyrimidin-4-amine; 3-(8-Chloro-3-((1R)-1-((pyrido(3,2-d)pyrimidin-4-yl)amino)-2,2,2-trifluoroethyl)quinolin-2-yl)pyridine N-oxide; N-((R)-1-(8-Chloro-2-(1-oxopyridin-3-yl)quinolin-3-yl)-2,2,2-trifluoroethyl)pyrido(3,2-d)pyrimidin-4-ylamine; Pyrido(3,2-d)pyrimidin-4-amine, N-((1R)-1-(8-chloro-2-(1-oxido-3-pyridinyl)-2,2,2-trifluoroethyl)-; seletalisibum; 3-(8-chloro-3-((1R)-2,2,2-trifluoro-1-((pyrido(3,2-d)pyrimidin-4-yl)amino)ethyl)quinolin-2-yl)pyridin-1-ium-1-olate; 3-{8-chloro-3-[(1R)-2,2,2-trifluoro-1-({pyrido[3,2-d]pyrimidin-4-yl}amino)ethyl]quinolin-2-yl}pyridin-1-ium-1-olate; N-(1-(8-chloro-2-(1-oxidopyridin-1-ium-3-yl)-3-quinolyl)-2,2,2-trifluoroethyl)pyrido(3,2-d)pyrimidin-4-amine; N-[(1R)-1-[8-chloro-2-(1-oxidopyridin-1-ium-3-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine; (R)-3-(8-Chloro-3-(2,2,2-trifluoro-1-(pyrido[3,2-d]pyrimidin-4-ylamino)ethyl)quinolin-2-yl)pyridine 1-oxide
- 用途
- Seletalisib是新型PI3Kδ小分子抑制剂，IC50为12 nM，对PI3Kδ选择性高24-303倍；在B细胞中阻止AKT/PKB磷酸化，抑制N-甲酰肽段刺激的超氧化物释放，抑制活化T细胞细胞因子生成及B细胞增殖，抑制B细胞活化CD69表达和嗜碱性细胞脱粒；在Ramos细胞中抑制AKT磷酸化IC50为15 nM；在大鼠体内抑制IL-2释放IC50<10 nM；首次人体试验显示血浆浓度时间分布与剂量比例偏差小，无蓄积或暴露缺失，半衰期约20小时。
