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Version: 16.11d (Release date: 2016-11-28)
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Diazepinomicin (Code C62508)

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Terms & Properties

Preferred Name: Diazepinomicin

Definition: A potent inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Diazepinomicin binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2), that play a crucial role in regulating cell growth and survival. Diazepinomicin also selectively binds to the peripheral benzodiazepine receptor (BZRP), a receptor highly expressed in certain cancer cells, thus inducing cell cycle arrest and apoptosis in BZRP-expressing cells. In addition, diazepinomicin is able to cross the blood-brain barrier, thereby reaching therapeutic concentrations in the brain.

Display Name: Diazepinomicin

Label: Diazepinomicin

NCI Thesaurus Code: C62508 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1527794  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
11h-dibenzo(B,E)(1,4)diazepin-11-one, 5,10-dihydro-4,6,8-trihydroxy-10-((2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrien-1-yl)-
BU-4664L
Diazepinomicin
DIAZEPINOMICIN
ECO-4601
TLN-4601

External Source Codes: 
CAS Registry Number 733035-26-2 (see NLM ChemIDplus info)
CAS Registry Number C28H34N2O4 (see NLM ChemIDplus info)
FDA UNII Code YPH994Y0RF
PDQ Closed Trial Search ID 496938
PDQ Open Trial Search ID 496938 (check for NCI PDQ open clinical trial info)
PubMedID Primary Reference 20655882 (see PubMed Primary Reference info)
UMLS CUI C1527794

Other Properties:
Name Value (qualifiers indented underneath)
code C62508
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name ECO-4601
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=C62508

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