Preferred Label : Telaglenastat Hydrochloride;
NCIt synonyms : CB-839 HCl; 2-Pyridineacetamide, N-(5-(4-(6-((2-(3-(trifluoromethoxy)phenyl)acetyl)amino)-3-pyridazinyl)butyl)-1,3,4-thiadiazol-2-yl)-,
Hydrochloride (1:1); Glutaminase Inhibitor CB-839 Hydrochloride;
NCIt definition : The hydrochloride salt form of CB-839, an orally bioavailable inhibitor of glutaminase,
with potential antineoplastic and immunostimulating activities. Upon oral administration,
CB-839 selectively and reversibly binds to and inhibits human glutaminase, an enzyme
that is essential for the conversion of the amino acid glutamine into glutamate. Blocking
glutamine metabolism inhibits proliferation in rapidly growing tumor cells and leads
to an induction of cell death. Unlike normal healthy cells, glutamine-dependent tumors
heavily rely on the intracellular conversion of exogenous glutamine into glutamate
and glutamate metabolites to both provide energy and generate building blocks for
the production of macromolecules, which are needed for cellular growth and survival.
In addition, CB-839 causes accumulation of glutamine in tumor cells and increases
glutamine concentration in the tumor microenvironment (TME) upon cell death. As glutamine
is essential for T-cell generation, CB-839 may also enhance T-cell proliferation and
activation in the TME, which may lead to further killing of tumor cells.;
UNII : B33561JJ61;
InChIKey : NMVMURBPQFKTAX-UHFFFAOYSA-N;
CAS number : 1874231-60-3; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1874231-60-3
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G-SRS /a ;
NCI Metathesaurus CUI : CL552142;
Origin ID : C150413;
UMLS CUI : C5418246;
Semantic type(s)
- concept_is_in_subset
- has_target
