TSU-68

TSU-68 (SU6668) is an oral tyrosine kinase inhibitor of VEGFR-2, PDGFR and FGFR. TSU-68 inhibits SCF-induced proliferation of MO7E cells with IC50 of 0.29 μM, and induces apoptosis. TSU-68 (SU6668) also inhibits Aurora kinases B and C (IC50 = 35 and 210 nM respectively). TSU68 suppresses tumor growth, blocks angiogenesis in tumors, and induces apoptosis of tumor vasculature and regression of established tumors. In a tumor model of HT29 human colon carcinoma, TSU-68 (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core.