AFP464
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AFP464 Definition
A synthetic, lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and anti-tumor activities. AFP464 is rapidly converted to the aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in CYP1A1 enzyme activity and, to a lesser extent, an increase in CYP1B1 enzyme activity and gene expression. Subsequently, aminoflavone is metabolized by the CYP1A1 and CYP1B1 enzymes that it induces. Toxic metabolites of aminoflavone covalently bind to DNA, thereby inhibiting cell proliferation and inducing apoptosis. Pulmonary toxicity may be a dose-limiting toxicity.
AFP464 Synonyms
AFP464
Terms in AFP464 category
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