AFP-464

AFP-464 is a synthetic lysyl prodrug of the amino-substituted flavone derivative aminoflavone, developed as an antitumor agent. It acts primarily by activating the aryl hydrocarbon receptor (AhR) signaling pathway, leading to its conversion into metabolites that covalently bind DNA, resulting in p53 activation and apoptosis. This mechanism produces antiproliferative and antineoplastic effects, particularly in estrogen receptor-positive (ER+) breast cancer. Preclinical studies have shown that tumors with cytoplasmic AhR localization are especially sensitive to AFP-464. The drug has demonstrated growth inhibitory activity against breast, ovarian, lung, and renal tumor cell lines and has shown efficacy in xenograft models for renal and breast cancers. Additionally, it may enhance anti-tumor immune responses by modulating macrophage phenotypes and reducing immunosuppressive cells within the tumor microenvironment[1][2][4][5][6].

Other names

aminoflavone prodrug AFP464lysyl prodrug of aminoflavoneAFP464 free baseAFP-464 free baseAFP 464 free base