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| Product | Description | |
|---|---|---|
| Tazemetostat hydrobromide | Tazemetostat hydrobromide is a potent, selective and orally bioavailable EZH2 inhibitor with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. It inhibits EZH1 and rat EZH2 with IC50s of 392 nM and 4 nM, respectively. It inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Group: Pharmaceutical. Alternative Names: EPZ-6438 hydrobromide; E-7438 hydrobromide; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-, hydrobromide (1:1); 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 hydrobromide. CAS No. 1467052-75-0. Pack Sizes: 100 mg. Product ID: B1370-382050. Molecular formula: C34H45BrN4O4. Mole weight: 653.65. Custom synthesis is available. Send your inquiries for more information. |  London |
| EPZ-6438 | 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. Group: Pharmaceutical. Alternative Names: EPZ-6438; EPZ 6438; EPZ6438; E7438; E-7438; E 7438; Tazemetostat. CAS No. 1403254-99-8. Pack Sizes: 1 g. Product ID: B0084-462339. Molecular formula: C34H44N4O4. Mole weight: 572.75. Custom synthesis is available. Send your inquiries for more information. | London |
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