Potent and selective EZH2 inhibitor
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
.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-168456 |
| Réf. fabricant | 30226368 |
| Nom chimique ou matériau | 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 |
| CAS | 1403254-99-8 |
| Quantité | 10 mg |
| Cible | EZH2 Inhibitor |
| Formule moléculaire | C34H44N4O4 |
| Pureté | 0.97 |
