Tazemetostat (EPZ-6438) - 99%, high purity , CAS No.1403254-99-8, Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit

Item Number

T413712

• Synonyms: HMS3653O07 | Tazemetostat [USAN:INN] | Tazemetostatum | BCP07409 | HMS3747A09 | SW220030-1 | 5-(Ethyl(tetrahydro-2H-pyran-4-yl)amino)-N-((2-hydroxy-4,6-dimethylpyridin-3-yl)methyl)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide | N-[(4,6-Dim
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with K_i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit
• Note: 10mg卖完停产，不再备货

Product Description

Information

Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with K i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

Targets

EZH2 (Cell-free assay) 2.5 nM(Ki)

In vitro

EPZ-6438 concentration-dependently reduces global H3K27Me3 levels in wild-type or SMARCB1 mutant cells, and induces strong antiproliferative effects with IC50 ranging from 32 nM to 1000 nM in SMARCB1-deleted MRT cell lines. EPZ-6438 induces gene expression of neuronal differentiation and cell cycle inhibition, while inhibtis expression of Hedgehog pathway genes, MYC and EZH2. The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines.

In vivo

In SCID mice bearing s.c. G401 xenografts, EPZ-6438 induces tumor stasis during the administration period and produces a significant tumor growth delay with minimal effect on body weight.

Cell Research(from reference)

Cell lines：Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30) 

Concentrations：~10 μM 

Incubation Time：7 days