Preferred Name

Telaglenastat Hydrochloride

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C150413

CAS_Registry

1874231-60-3

code

C150413

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C177537

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C63923

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978

Contributing_Source

CTRP

GDC

FDA

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.

Display_Name

Telaglenastat Hydrochloride

FDA_UNII_Code

B33561JJ61

FULL_SYN

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

TELAGLENASTAT HYDROCHLORIDE

CB-839 HCl

Telaglenastat Hydrochloride

Has_Target

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128179

Is_Value_For_GDC_Property

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1909

label

Telaglenastat Hydrochloride

Maps_To

Glutaminase Inhibitor CB-839 Hydrochloride

Telaglenastat Hydrochloride

NCI_Drug_Dictionary_ID

801359

NCI_META_CUI

CL552142

PDQ_Closed_Trial_Search_ID

801359

PDQ_Open_Trial_Search_ID

801359

Preferred_Name

Telaglenastat Hydrochloride

prefixIRI

Thesaurus:C150413

prefLabel

Telaglenastat Hydrochloride

Semantic_Type

Pharmacologic Substance

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C471

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