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Formula | C34H44N4O4 |
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Molecular Weight | 572.74 | CAS No. | 1403254-99-8 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (174.59 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Tazemetostat (EPZ-6438, E7438) 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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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 NSC-9900 or Hexadecadrol in several EZH2 mutant lymphoma cell lines. [2] |
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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] |
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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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Data from [Data independently produced by , , Cell, 2018, 175(1):186-199]
Data from [Data independently produced by , , J Pathol, 2017, 242(3):371-383]
Data from [Data independently produced by , , Clin Epigenetics, 2018, 10(1):121]
Data from [Data independently produced by , , Oncotarget, 2016, 7(10):11194-207]
AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6] | PubMed: 39385030 |
EZH2 inhibitors promote β-like cell regeneration in young and adult type 1 diabetes donors [ Signal Transduct Target Ther, 2024, 9(1):2] | PubMed: 38161208 |
Epigenetic regulation of CD38/CD48 by KDM6A mediates NK cell response in multiple myeloma [ Nat Commun, 2024, 15(1):1367] | PubMed: 38355622 |
Interferon-induced factor 16 is essential in metastatic melanoma to maintain STING levels and the immune responses upon IFN-γ response pathway activation [ J Immunother Cancer, 2024, 12(10)e009590] | PubMed: 39424359 |
Epigenetic dysregulation of eukaryotic initiation factor 3 subunit E (eIF3E) by lysine methyltransferase REIIBP confers a pro-inflammatory phenotype in t(4;14) myeloma [ Haematologica, 2024, 109(6):1893-1908] | PubMed: 38124661 |
C-terminal binding protein (CTBP2) is a novel tumor suppressor targeting the MYC-IRF4 axis in multiple myeloma [ Blood Adv, 2024, bloodadvances.2023010218] | PubMed: 38457926 |
Interferon regulatory factor 4 modulates epigenetic silencing and cancer-critical pathways in melanoma cells [ Mol Oncol, 2024, 10.1002/1878-0261.13672] | PubMed: 38880659 |
Isothiocyanates Potentiate Tazemetostat-Induced Apoptosis by Modulating the Expression of Apoptotic Genes, Members of Polycomb Repressive Complex 2, and Levels of Tri-Methylating Lysine 27 at Histone 3 in Human Malignant Melanoma Cells [ Int J Mol Sci, 2024, 25(5)2745] | PubMed: 38473991 |
PDGF-BB overexpression in p53 null oligodendrocyte progenitors increases H3K27me3 and induces transcriptional changes which favor proliferation [ Neoplasia, 2024, 57:101042] | PubMed: 39216363 |
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors [ J Biol Chem, 2024, 300(10):107765] | PubMed: 39276936 |
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