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Tazemetostat

Inh 1403254-99-8 N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
N° du produit ABIN7233296
  • Application
    Inhibition (Inh)
    Fonction
    EZH2 inhibitor
    Attributs du produit
    Potent and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2 (Ki = 2.5nM wild type human PRC2-containing). Displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines in vitro. Antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. Displays potent antitumor activity in various cancer models including non-Hodgkins lymphoma, pediatric glioma, small-cell carcinoma of the ovary, and synovial sarcomas. Tazemetostat has also been shown to control inflammatory genes by modulating IRF1, IRF8, and STAT1 levels suggesting therapeutic potential for the treatment of neuroinflammatory diseases associated with microglial activation.
    Pureté
    >98 %
    Chemical Name
    N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
    Formula
    C34H44N4O4
    Solubility
    Soluble in DMSO (up to at least 25 mg/ml)
  • Restrictions
    For Research Use only
  • Format
    Powder
    Stock
    -20 °C
  • Sujet
    EPZ-6438,Transcription,Epigenetics,Proliferation,Protein methyltransferase,Cancer stem cells,Inflammation,Cancer,Posttranslational modification,Neurodegeneration,Chromatin
    Poids moléculaire
    572.75
    Numéro CAS
    1403254-99-8
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