Tazemetostat(EPZ-6438) chemical structure

Chemical structureResearch use only

CAT. NO. DC7122Featured

Tazemetostat(EPZ-6438)

Name: Tazemetostat(EPZ-6438)
Brand: DC Chemicals
SKU: DC7122
Price: 350.0 USD

Pack Sizes & Prices

TotalUS$350

We match the best price and quality on market.

Product overview

Description & Application

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

Parameter	Value
Chemical Name	Tazemetostat free base
CAS No.	1403254-99-8
Synonyms	N-[(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
Formula	C34H44N4O4
M.Wt	572.74
SMILES	O1C([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%
Storage	2 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.

Product documentation

View online datasheet Request COA / MSDS

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

Related research products

DC6308

Sofosbuvir（PSI7977，GS-7977）

Sofosbuvir (PSI-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM.

View activity & prices

DC22228

Fluzoparib

Fluzoparib (SHR-3162) is a novel, potent and orally available inhibitor of PARP; potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination…

View activity & prices

DC7101

CGK733

CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.

View activity & prices

DC2086

PF-670462

PF-670462 is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

View activity & prices

DC7550

PBIT

PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1(JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1 ) histone demethylase an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with…

View activity & prices

DC60394

PU-WS13

PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 μM.

View activity & prices

DC7071

AWD 131-138(Imepitoin)

AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

View activity & prices

DC7035

Merestinib(LY2801653 dihydrochloride)

Merestinib dihydrochloride (LY2801653 dihydrochloride) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM.

View activity & prices

DC9424

Fenoldopam (mesylate)

Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with…

View activity & prices