DMXAA acts as a tumor vascular disrupting agent, inducing apoptosis in tumor vascular endothelium resulting in necrosis at the tumor core. It potently activates the TANK-binding kinase 1-interferon regulatory factor 3 signaling pathway in leukocytes, inducing type-I-interferon production. In addition, DMXAA significantly inhibits several kinases in endothelial cells, including the vascular endothelial growth factor (VEGF) receptors VEGFR1 and VEGFR2 (IC₅₀ = 119 and 11 µM, respectively). Recent studies have shown that DMXAA is a competitive agonist ligand for mouse.