|AFP464 (Code C48370)|
|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
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)|
|Name||Value (qualifiers indented underneath)|
Additional Concept Data:
|Defined Fully by Roles: No|