Preferred Label : Tulmimetostat;
NCIt synonyms : EZH2 Inhibitor CPI-0209; 1,3-Benzodioxole-5-carboxamide, 7-chloro-N-((1,2-dihydro-6-methyl-4-(methylthio)-2-oxo-3-pyridinyl)methyl)-2-(trans-4-(3-methoxy-1-azetidinyl)cyclohexyl)-2,4-dimethyl-,
(2R)-;
NCIt definition : An orally available selective inhibitor of the histone lysine methyltransferase (HMT)
enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral
administration, tulmimetostat selectively targets, binds to and inhibits the activity
of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on
lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns
associated with cancer pathways and results in decreased proliferation of EZH2-expressing
cancer cells. EZH2, an HMT class enzyme and the catalytic subunit of the polycomb
repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells
and plays a key role in tumor cell proliferation; its expression is correlated with
tumor initiation, progression, stem cell self-renewal, migration and angiogenesis.;
UNII : OUQ4N85Z0B;
CAS number : 2567686-02-4;
Molecule name : CPI 0209; CPI-0209;
NCI Metathesaurus CUI : CL972321;
Origin ID : C167347;
UMLS CUI : C5706577;
Semantic type(s)
- concept_is_in_subset
- has_target
