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National Cancer Institute
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Version: 17.12d (Release date: 2017-12-26)
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AFP464 (Code C48370)

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Terms & Properties

Preferred Name: AFP464

Definition: A synthetic lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and antineoplastic activities. AFP464 is rapidly converted to aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in cytochrome P450 1A1 (CYP1A1) and cytochrome P450 1A2 (CYP1A2) expression and, to a lesser extent, an increase in cytochrome P450 1B1 (CYP1B1) expression. Subsequently, aminoflavone is metabolized to toxic metabolites by the cytochromome P450 enzymes that it induces; these toxic metabolites covalently bind to DNA, resulting in the phosphorylation of p53, the induction of the p53 downstream target p21Waf1/Cip1, and apoptosis. Pulmonary toxicity may be dose-limiting.

NCI-GLOSS Definition: A substance being studied in the treatment of cancer. AFP464 kills cancer cells or stops them from dividing. It is a type of aminoflavone.

Display Name: AFP464

Label: AFP464

NCI Thesaurus Code: C48370 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1706653  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)

External Source Codes: 
PDQ Closed Trial Search ID 453584
PDQ Open Trial Search ID 453584 (check for NCI PDQ open clinical trial info)
UMLS CUI C1706653

Other Properties:
     Name Value (qualifiers indented underneath)
code C48370
Contributing_Source CTRP
Legacy_Concept_Name AFP464
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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