5F-203

5F-203 (NSC-703786) is an experimental cytotoxic small molecule and antitumor agent. It acts as a potent ligand and agonist of the aryl hydrocarbon receptor (AhR). Upon binding to AhR, the complex translocates to the nucleus and induces the expression of cytochrome P450 enzymes, particularly CYP1A1 and CYP2W1. These enzymes metabolize 5F-203 into electrophilic reactive intermediates (such as nitrenium species) that form DNA adducts, leading to DNA double-strand breaks, replication stress, cell cycle arrest, and apoptosis. 5F-203 has demonstrated selective and potent antitumor activity in preclinical models of breast, ovarian, renal, and gastric cancers. A water-soluble lysylamide prodrug of 5F-203, known as Phortress (NSC-710305), was developed to improve solubility and advanced into Phase 1 clinical trials.

Other names

2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole4-(5-fluorobenzo[d]thiazol-2-yl)-2-methylaniline5F 2035F203