EPZ6438

EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2. It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases. EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM). EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and to promote their regression in xenograft-bearing mice.Formal Name: 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)-[1,1'-biphenyl]-3-carboxamide. CAS Number: 1403254-99-8. Synonyms: Tazemetostat. Molecular Formula: C34H44N4O4. Formula Weight: 572.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml. lambdamax: 256 nm. SMILES: CC(C(N(C1CCOCC1)CC)=C2)=C(C(NCC3=C(C)C=C(C)NC3=O)=O)C=C2C4=CC=C(CN5CCOCC5)C=C4. InChi Code: InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40). InChi Key: NSQSAUGJQHDYNO-UHFFFAOYSA-N.