Acriflavine is identified as a potent inhibitor of the MCT4 that can inhibit the binding between Basigin and MCT4. Acriflavine significantly inhibits growth and self-renewal potential of several glioblastoma neurosphere lines. The HIF-1 inhibitor acriflavine decreases survival and growth of CML cells. It targets stem cell potential of CML cells.

Acriflavine treatment inhibits intratumoral expression of VEGF and tumor vascularization. In a murine CML model, acriflavine decreases leukemia development and reduces LSC maintenance. Acriflavine retards tumor growth in a murine model of breast cancer. The combination of sunitinib with acriflavine significantly decreases vascular endothelial growth factor and TGF-β expression and reduces tumor vasculature followed by increased intratumor necrosis and apoptosis.