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Version: 17.12d (Release date: 2017-12-26)
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Apaziquone (Code C1087)

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Terms & Properties

Preferred Name: Apaziquone

Definition: An indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. The active metabolites alkylate DNA, resulting in apoptotic cell death. This agent displays selectivity activity towards both hypoxic solid tumors, which exhibits higher expression of cytochrome P450 reductase, and well-oxygenated malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase). Apaziquone may selectively sensitize hypoxic tumor cells to radiocytotoxicity.

Display Name: Apaziquone

Label: Apaziquone

NCI Thesaurus Code: C1087 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C0095568  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
3-hydroxymethyl-5-aziridinyl-1-methyl-2-(1H-indole-4,7-dione) prop-beta-en-alpha-ol
E O9

External Source Codes: 
CAS Registry Number 114560-48-4 (see NLM ChemIDplus info)
FDA UNII Code H464ZO600O
NSC Code 382456 (see NCI DTP info)
PDQ Closed Trial Search ID 42095
PDQ Open Trial Search ID 42095 (check for NCI PDQ open clinical trial info)
UMLS CUI C0095568

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C15H16N2O4
code C1087
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name EO9
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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