Tazemetostat(EPZ-6438) Datasheet DC Chemicals
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Cat.No DC7122
Name Tazemetostat(EPZ-6438)

Chemical Properties

CAS 1403254-99-8
Formula C34H44N4O4
MW 572.7376
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description CAS NO.：1403254-99-8
Product Name：Tazemetostat
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
EINEC:
Molecular Formula：C34H44N4O4
Molecular Weight：572.7376
Target:
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].
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].
Kinase Assay
Cell Assay
Animal Administration

References

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