EPZ-6438

Overview

EPZ-6438 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. EPZ-6438 is currently in clinical trials.

Application

Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cancer | EZH2

Product Information

• Catalog No.: B0084-462339
• CAS No.: 1403254-99-8
• Molecular Formula: C34H44N4O4
• Molecular Weight: 572.75
• Purity: 98%
• Storage: 2 - 8 °C

Source

Original product source