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

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide Structure
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide structure
Common 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
CAS Number 2238820-26-1 Molecular Weight 542.67
Density N/A Boiling Point N/A
Molecular Formula C32H38N4O4 Melting Point N/A
MSDS N/A Flash Point N/A

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


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.

 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
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