AG311 is a small molecule inhibitor of complex I and hypoxia-induced HIF-1α stabilization. In vitro, AG311 induces rapid necrosis in numerous cancer cell lines. Within minutes, exposure to AG311 also results in mitochondrial depolarization, superoxide production, and increased intracellular calcium levels. AG311 retards tumor growth and reduces lung metastases better than clinically used agents and has no gross or histopathological toxicity. AG311 is a first-in-class antitumor and antimetastatic agent inducing necrosis in breast cancer tumors, likely through the mitochondria.
