 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1403254-99-8 |
| Molecular formula(MF) | C34H44N4O4 |
| Molecular Weight(MW): | 572.74 |
| Alias | EPZ-6438; E-7438; EPZ-7438 |
| In vitro | DMSO | 5 mg/mL warmed (8.72 mM) |
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| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL | |
| In vivo | 4% DMSO+30% PEG 300+5% Tween 80+ddH2O | 2.5mg/mL |
| 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. | ||||||||||||||||
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| 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. | ||||||||||||||||
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| 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. [1] The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines. [2] |
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| Cell Data |
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| 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. [1] |