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Version: 17.06d (Release date: 2017-06-26)
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Tazemetostat (Code C107506)

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Terms & Properties

Preferred Name: Tazemetostat

Definition: An orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation.

Display Name: Tazemetostat

Label: Tazemetostat

NCI Thesaurus Code: C107506 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3827128  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
E7438
EPZ-6438
EPZ6438
N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide
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
Tazemetostat
TAZEMETOSTAT

External Source Codes: 
CAS Registry Number 1403254-99-8 (see NLM ChemIDplus info)
FDA UNII Code Q40W93WPE1
PDQ Closed Trial Search ID 751383
PDQ Open Trial Search ID 751383 (check for NCI PDQ open clinical trial info)
UMLS CUI C3827128

Other Properties:
     Name Value (qualifiers indented underneath)
code C107506
Contributing_Source CTRP
Contributing_Source FDA
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C107506

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