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

Names

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

Biological Activity

[Description]:

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide is a potent and selective Enhancer of Zeste Homolog 2 (EZH2) inhibitor with IC50 0f 37.6 nM and 79.1 nM for EZH2 WT and EZH2-Y641F, respectively.

[In Vitro]

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide exhibits antiproliferative effects against the WSU-DLCL2 cell line with GI50 of 0.2 μM.

[References]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₈N₄O₄

[ Molecular Weight ]:
542.67

Related Compounds

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