Tazemetostat New
Chemical Name: 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
Purity: ≥97%
Biological Activity
Tazemetostat is a potent and selective EZH2 inhibitor (Ki = 2.5 nM; IC50 = 11 nM). Reduces H3K27me3 levels in PDX derived cells and inhibits cellular H3K27 methylation. Tazemetostat suppresses EZH2 and MYC expression and induces neuronal differentiation genes; also increases neurite extension in MB-39-nu cells. Antiproliferative in SMARCAB1-deleted MRT cell lines (IC50 = 32 - 1000 nM); inhibits methylation in both mutant and wild type cells (IC50 = 1.4-4.9 nM). Dose-dependently suppresses growth of both MC38 cells and tumors in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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