EPZ-6438 (Tazemetostat)Catalog No. A12712

Quick Overview

EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
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EPZ-6438 (Tazemetostat)

EPZ-6438 (Tazemetostat)  Citations(2)
  • Wang Z, .et al. Targeting EZH 2 as a novel therapeutic strategy for sorafenib-resistant thyroid carcinoma, J Cell Mol Med, 2019, May 13 PMID: 31087496
  • Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
  • Product Information
    Catalog Num A12712
    M. Wt 572.74
    Formula C34H44N4O4
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 1403254-99-8
    Synonyms EPZ6438, EPZ 6438
    SMILES Code CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5

    Biological activity
    Introduction
    EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
    Targets
    EZH2 (Cell-free assay) EZH2 (Cell-free assay)
    2.5 nM(Ki)2.5 nM(Ki)
    Solubility
    Solubility (25C)* In vitro DMSO 29 mg/mL (50.63 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq 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.
    Return Policy Contact information
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