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Tazemetostat(EPZ-6438) — Datasheet

CAT. NO. DC7122

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ParameterValue
Chemical NameTazemetostat free base
CAS No.1403254-99-8
SynonymsN-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide;EPZ-6438;E-7438;EPZ-7438;EPZ 6438;EPZ-6438 (E-7438);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;Tazemetostat;Tazemetostat (EPZ-6438);EPZ-6438 (E7438);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;S7128,E7438;EPZ6438;Q40W93WPE1;E7438;(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)-;N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(m
FormulaC34H44N4O4
M.Wt572.74
SMILESO1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N(C([H])([H])C([H])([H])[H])C1=C([H])C(C2C([H])=C([H])C(=C([H])C=2[H])C([H])([H])N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])=C([H])C(C(N([H])C([H])([H])C2C(N([H])C(C([H])([H])[H])=C([H])C=2C([H])([H
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor with Ki and IC50 of 2.5 and 11 nM, respectively.

In Vitro

Tazemetostat (EPZ-6438) inhibits EZH2 in a manner competitive with the substrate S-adenosylmethionine (SAM). Tazemetostat inhibits EZH1, EZH2(in peptide assay), EZH2 (in nucleosome assay) with IC50of 392 nM, 11 nM and 16 nM, respectively. Tazemetostat displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs tested[1].

In Vivo

Tazemetostat (EPZ-6438, 125 mg/kg) induces tumor stasis during the administration period and produced a significant tumor growth delay compared with vehicle after the dosing period. Measuring Tazemetostat plasma levels either 5 min before or 3 h after dosing on day 21 reveals a clear dose-dependent increase in systemic exposure[1]. Dose-dependent target inhibition is observed in PBMCs and bone marrow from rats dosed with Tazemetostat (EPZ-6438, orally administered, 100, 300, or 1,000 mg/kg) as measured by ELISA[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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