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Version: 17.06d (Release date: 2017-06-26)
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Ganetespib (Code C77872)

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Terms & Properties

Preferred Name: Ganetespib

Definition: A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Ganetespib binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.

Display Name: Ganetespib

Label: Ganetespib

NCI Thesaurus Code: C77872 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C2607234  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
3-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4h-1,2,4-triazole 3h-1,2,4-triazol-3-one
5-(2,4-dihydroxy-5-(1-methylethyl)phenyl)-2,4-dihydro-4-(1-methyl-1h-indol-5-yl)-
Ganetespib
GANETESPIB
Hsp90 Inhibitor STA-9090
STA-9090

External Source Codes: 
CAS Registry Number 1143571-94-1 (see NLM ChemIDplus info)
FDA UNII Code 2E8412Y946
PDQ Closed Trial Search ID 598379
PDQ Open Trial Search ID 598379 (check for NCI PDQ open clinical trial info)
UMLS CUI C2607234

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C20H20N4O3
code C77872
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name Hsp90_Inhibitor_STA-9090
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C77872

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