Catalog No.S7128 Synonyms: E7438
Molecular Weight(MW): 572.74
Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki 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.
2 Customer Reviews
we examined the E-cadherin, ZEB1 and Snail expressions after using EZH2 RNAi, DZNeP and EPZ-6438. “*”represent P<0.05 when compared with control group.
Oncotarget, 2016, 7(10):11194-207. Tazemetostat (EPZ-6438) purchased from Selleck.
EZH2 inhibition does not affect pediatric high-grade glioma cell growth in vitro. (a-c) Relative cell viability of pediatric high-grade glioma cell lines were subjected to MTT cell viability assays 72 h after incubation with increasing concentrations of Tazemetostat (EPZ-6438) as indicated. Graphs show the mean of 3 independent biological replicates with the respective SEM, * p < 0.05.
Klin Padiatr, 2016, 228(3):113-117.. Tazemetostat (EPZ-6438) purchased from Selleck.
Purity & Quality Control
Choose Selective Histone Methyltransferase Inhibitors
|Description||Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki 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.|
|Features||Orally bioavailable EZH2-selective inhibitor for both wild-type and mutant. Currently being tested in Phase II clinical trials for treatment of Diffuse Large B Cell Lymphoma.|
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. |
Biochemical Methods:EPZ-6438 is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions’’. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
|In vitro||DMSO||5 mg/mL warmed (8.72 mM)|
|In vivo||4% DMSO+30% PEG 300+5% Tween 80+ddH2O||2.5mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01897571||Recruiting||B-cell Lymphomas (Phase 1)|Advanced Solid Tumors (Phase 1)|Diffuse Large B-cell Lymphoma (Phase 2)|Follicular Lymphoma (Phase 2)|Transformed Follicular Lymphoma|Primary Mediastinal Large B-Cell Lymphoma||Epizyme, Inc.||June 2013||Phase 1|Phase 2|
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