ODM-203

A dual inhibitor of VEGFR and FGFR (IC50s = 5-26 and 6-35 nM for VEGFR1-3 and FGFR1-4, respectively); selective for VEGFR1-3 and FGFR1-4 over a panel of 308 kinases at 1 µM; inhibits PDGFRα, PDGFRβ, and DDR1 (IC50s = 35, 169, and 6 nM, respectively), as well as MAP4K4, MINK1, RET, SIK2, YES1, and Tie2 (IC50s = 49, 41, 8, 23, 152, and 174 nM, respectively; inhibits FGFR-dependent proliferation in H1581 lung, SNU-16 stomach, and RT4 bladder cancer cells (IC50s = 104, 132, and 192 nM, respectively) and VEGF-induced tube formation by HUVECs (IC50 = 33 nM); decreases tumor volume in a RT4 mouse xenograft model at 20 and 40 mg/kg; reduces tumor growth and intratumor phosphorylation of FGFR in a SNU-16 mouse xenograft model at 30 mg/kg