AG311

AG311 is a preclinical multi-targeted small molecule inhibitor designed to target both tumor metabolism and angiogenesis. It competitively inhibits Complex I (NADH:ubiquinone oxidoreductase) of the mitochondrial electron transport chain at the ubiquinone-binding site, leading to mitochondrial depolarization, ATP depletion, and necrotic cell death, particularly under hypoxic conditions. Additionally, AG311 inhibits receptor tyrosine kinases (including EGFR, VEGFR-2, and PDGFR-β) and thymidylate synthase (TS), combining antiangiogenic and cytotoxic mechanisms. Developed by Duquesne University in collaboration with the University of Oklahoma Health Sciences Center and the Oklahoma Medical Research Foundation, AG311 has demonstrated significant antitumor and antimetastatic activity in preclinical models of triple-negative breast cancer.

Other names

5-[(4-methylphenyl)sulfanyl]-9H-pyrimido[4,5-b]indole-2,4-diamine5-[(4-methylphenyl)thio]-9H-pyrimido[4,5-b]indole-2,4-diamine