Preferred Label : Aminoflavone Prodrug AFP464;
NCIt related terms : AFP464; AFP-464;
NCIt 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.;
Alternative definition : NCI-GLOSS: A substance being studied in the treatment of cancer. AFP464 kills cancer
cells or stops them from dividing. It is a type of aminoflavone.;
UNII : 73JNH95XPX;
CAS number : 468719-53-1;
Codes from synonyms : CDR0000514448;
Origin ID : C48370;
UMLS CUI : C1706653;
Semantic type(s)
- concept_is_in_subset
