N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide

• 常用名: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide
• 英文名: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide
• CAS号: 2238820-26-1
• 分子量: 542.67
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₂H₃₈N₄O₄
• 熔点: N/A
• 闪点: N/A

用途

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide 是一种强效的、选择性的Enhancer of Zeste Homolog 2 (EZH2),对EZH2 WT 和EZH2-Y641F 的IC50分别为37.6nM 和79.1nM。

名称

• 英文名: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide

生物活性

• 描述: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide 是一种强效的、选择性的Enhancer of Zeste Homolog 2 (EZH2),对EZH2 WT 和EZH2-Y641F 的IC50分别为37.6nM 和79.1nM。
• 体外研究: N-(4,6-二甲基-2-氧代-1,2-二氢吡啶-3-基)甲基)-5-(N-乙基环丙烷甲酰胺)-4-甲基-4′-吗啉基-[1,1′-联苯基]-3-甲酰胺对WSU-DLCL2细胞系具有抗增殖作用,GI50为0.2μM。
• 参考文献: 1. Zhou B, et al. Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas. J Med Chem. 2021 Oct 28;64(20):15170-15188.

物理化学性质

• 分子式: C₃₂H₃₈N₄O₄
• 分子量: 542.67