For R&D use only.

EPZ-6438

  • Catalog NO.:A857028
  • CAS No. : 1403254-99-8
  • Molecular Formula:C34H44N4O4
  • Molecular Weight: 572.74
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Quality Control&SDS
COA NMR

Product Details

CAS Number 1403254-99-8 Appearance Off-white powder
Catalog Number A857028 MDL Number MFCD24849415
Molecular Formula C34H44N4O4 Molecular Weight 572.74
Boiling Point Melting Point
Flash Point Density
Synonyms N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
Storage Condition Store in a tightly closed container,in a cool and dry place

Safety

GHS Pictogram
Signal Word Warning UN Number
Hazard Statements H302-H315-H319-H335 Class
Precautionary Statements P261-P305+P351+P338 Packing Group

Description

Tazemetostat, also known as EPZ-6438 and E7438, is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation. These data demonstrate the dependency of SMARCB1 mutant MRTs on EZH2 enzymatic activity and portend the utility of EZH2-targeted drugs for the treatment of these genetically defined cancers.

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EPZ-6438
N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide