Preferred Label : IDH1 Inhibitor KY100001;
NCIt synonyms : Mutant IDH1 Inhibitor KY100001; Mutant-selective IDH1 Inhibitor KY100001;
NCIt definition : An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1
[NADP ] soluble) mutant forms, with potential antineoplastic activity. Upon administration,
IDH1 inhibitor KY100001 specifically binds to and inhibits certain mutant forms of
IDH1, 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 IDH1 mutations. IDH1 mutations are highly expressed in certain
malignancies; they initiate and drive cancer growth by both blocking cell differentiation
and catalyzing the formation of 2HG.;
Molecule name : KY-100001; KY 100001;
NCI Metathesaurus CUI : CL1663469;
Origin ID : C180834;
UMLS CUI : C5556657;
Semantic type(s)
- concept_is_in_subset
- has_target
