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An Entity of Type : owl:Class, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
rdfs:label
  • Diazepinomicin
rdfs:subClassOf
Has_Target
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Diazepinomicin
PubMedID_Primary_Reference
  • 20655882
UMLS_CUI
  • C1527794
CAS_Registry
  • 733035-26-2
  • C28H34N2O4
In_Clinical_Trial_For
  • glioblastoma multiforme
FDA_UNII_Code
  • YPH994Y0RF
Contributing_Source
  • FDA
PDQ_Open_Trial_Search_ID
  • 496938
PDQ_Closed_Trial_Search_ID
  • 496938
Legacy_Concept_Name
  • ECO-4601
FULL_SYN
  • DIAZEPINOMICINPTFDAYPH994Y0RF
  • DiazepinomicinPTNCI
  • 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)-SNNCI
  • ECO-4601CNNCI
  • BU-4664LCNNCI
  • TLN-4601CNNCI
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.NCI
code
  • C62508
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