In Vitro: ODM-203 (eight-dose concentration series up to 3 μM; 96 h) potently inhibits FGFR signaling and proliferation in several FGFR-dependent cell lines. ODM-203 (eight-dose concentration series up to 3 μM; 10 days) inhibits endothelial tubule formation. ODM-203 (1, 10, 100, 1000 nM; 1 h) inhibiting FGFR and VEGFR cellular signaling in HUVEC cells.
In Vivo: ODM-203 (20, 40 mg/kg; p.o.; single daily for 21 days) inhibits FGFR phosphorylation and tumor growth in several FGFR-dependent xenografts by suppressing FGFR signaling in tumors. ODM-203 (7, 20, 40 mg/kg; p.o.; single daily for 21 days) shows strong anti-tumor activity in a VEGFR-dependent angiogenic orthotopic syngenic model (Renca) and suppresses angiogenesis. ODM-203 (20, 40 mg/kg; p.o.; single daily for 5 days) activates immune response in the tumor microenvironment.