Preferred Label : IDH2 Mutant Inhibitor SH1573;
NCIt synonyms : mIDH2 Inhibitor SH1573; IDH2 R140Q Mutant Inhibitor SH1573;
NCIt definition : An orally bioavailable inhibitor of mitochondrial enzyme isocitrate dehydrogenase
type 2 (IDH2; IDH-2) R140Q mutant, with potential antineoplastic activity. Upon oral
administration, IDH2 mutant inhibitor SH1573 specifically inhibits mutant IDH2 (mIDH2)
R140Q protein, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate
(2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads
to both an induction of cellular differentiation and an inhibition of cellular proliferation
in tumor cells expressing mIDH2 R140Q. IDH2 is mutated in a variety of cancers, and
mutated IDH2 initiates and drives cancer growth by catalyzing the formation of 2HG
and blocking cell differentiation.;
Molecule name : SH 1573; SH-1573;
NCI Metathesaurus CUI : CL1663036;
Origin ID : C180425;
UMLS CUI : C5556355;
Semantic type(s)
- concept_is_in_subset
