1202759-32-7

• 常用中文名：CNX-774
• 常用英文名：CNX-774
• CAS号：1202759-32-7
• 分子式：C₂₆H₂₂FN₇O₃
• 分子量：499.496
• 相关类别： 生物化工 抑制剂 血管生成(Angiogenesis) BTK 抑制剂
• 发布时间：2017-01-06 22:21:37
• 更新时间：2026-07-08 06:43:34
• CNX-774是口服活性的高效Btk抑制剂,IC50< 1 nM,能与活性位点上的Cys-481形成配体导向的共价键。

名称

• 中文名: 4-[4-[[5-氟-4-[[3-[(1-氧代-2-丙烯-1-基)氨基]苯基]氨基]-2-嘧啶基]氨基]苯氧基]-N-甲基-2-吡啶甲酰胺
• 英文名: 4-{4-[(4-{[3-(Acryloylamino)phenyl]amino}-5-fluoro-2-pyrimidinyl) amino]phenoxy}-N-methyl-2-pyridinecarboxamide
• 中文别名: 4-[4-[[5-氟-4-[[3-[(1-氧代-2-丙烯-1; 4-(4-((4-((3-丙烯酰胺苯基)氨基)-5-氟嘧啶-2-基)氨基)苯氧基)-N-甲基吡啶酰胺; 抑制剂CNX-774; BTK抑制剂(CNX-774)
• 英文别名: CNX774; CNX; 4-(4-((4-((3-Acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamid; Coumarin,7-methoxy-3-phenyl-4-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl); 4-(4-((4-(acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamide; 4-(4-((4-((3-acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamide; CNX-774 //BP; 4-[4-[[5-Fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl-2-pyridinecboxamide; 4-{4-[(4-{[3-(Acryloylamino)phenyl]amino}-5-fluoro-2-pyrimidinyl) amino]phenoxy}-N-methyl-2-pyridinecboxamide; 2H-1-Benzopyran-2-one,7-methoxy-3-phenyl-4-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl); CNX-77; 2-Pyridinecboxamide, 4-[4-[[5-fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl; 7-Methoxy-3-phenyl-4-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)coumarin; CNX-774, 10 mM in DMSO; 4-[4-[[5-fluoro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]-N-methylpyridine-2-cboxamide; 4-(4-(4-(3-acrylamidophenylamino)-5-fluoropyrimidin-2-ylamino)phenoxy)-N-methylpicolinamide; 4-[4-[[5-Fluoro-4-[[3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-2-pyrimidinyl]amino]phenoxy]-N-methyl-2-pyridinecboxamide CNX-774; 4-{4-[(4-{[3-(Acryloylamino)phenyl]amino}-5-fluoro-2-pyrimidinyl)amino]phenoxy}-N-methyl-2-pyridinecarboxamide; 4-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-7-methoxy-3-phenyl-2H-chromen-2-one

物化性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₂₆H₂₂FN₇O₃
• 分子量: 499.496
• 精确质量: 499.176819
• PSA: 136.88000
• LogP: 3.15
• 外观性状: 粉末
• 折射率: 1.690
• 储存条件: -20℃

生物活性

• 描述: CNX-774是口服活性的高效Btk抑制剂,IC50< 1 nM,能与活性位点上的Cys-481形成配体导向的共价键。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> BTK
  研究领域 >> 癌症
• 参考文献:

  [1]. Akinleye A, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol. 2013 Aug 19;6:59.

  [2]. In Vitro Reactivity Assessment of Covalent Drugs Targeting Bruton's Tyrosine Kinase

安全

• 危害码 (欧洲): N