Preferred Label : Valemetostat Tosylate;
NCIt synonyms : 1,3-Benzodioxole-5-carboxamide, 7-Chloro-N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-2-(trans-4-(dimethylamino)cyclohexyl)-2,4-dimethyl-,
(2R)-, Compd. with 4-Methylbenzenesulfonate (1:1); DS-3201 Tosylate;
NCIt definition : The tosylate form of valemetostat, an orally available selective inhibitor of the
histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and 2 (EZH2),
with potential antineoplastic activity. Upon oral administration, valemetostat selectively
inhibits the activity of both wild-type and mutated forms of EZH1 and EZH2. Inhibition
of EZH1/2 specifically prevents the methylation of lysine 27 on histone H3 (H3K27).
This decrease in histone methylation alters gene expression patterns associated with
cancer pathways, enhances transcription of certain target genes, and results in decreased
proliferation of EZH1/2-expressing cancer cells. EZH1/2, histone lysine methyltransferase
(HMT) class enzymes and catalytic subunits of the polycomb repressive complex 2 (PRC2),
are overexpressed or mutated in a variety of cancer cells and play key roles in tumor
cell proliferation, progression, stem cell self-renewal and migration.;
UNII : 6N79I7X5II;
InChIKey : JSBKGJUYSLVFPF-WJQUPPJOSA-N;
CAS number : 1809336-93-3;
Drug name : Ezharmia;
Molecule name : DS 3201b; DS-3201b;
NCI Metathesaurus CUI : CL972910;
Origin ID : C168589;
UMLS CUI : C5238968;
Semantic type(s)
- concept_is_in_subset
- has_target
