Description
A PDGFR and FGFR inhibitor (IC50s = 5.35, 4.6, 28, 28, and 78 nM for PDGFRα, PDGFRβ, FGFR1, -2, and -3, respectively); selective for these kinases over FGFR4 (IC50 = >1,000 nM) but also inhibits c-Kit, VEGFR2, VEGFR1, and IGF-1R (IC50s = 67, 33, 36, and 75 nM, respectively), as well as EGFR, BTK, Cdk4/cyclin D3, and MET (IC50s = 128, 198, 214, and 396 nM, respectively); inhibits the proliferation of MG-63, U2OS, MNNG/HOS, and Saos-2 cells (IC50s = 0.84, 0.76, 1.36, and 0.72 µM, respectively); inhibits the migration and invasion of U87MG and LN-229 cells at 0.3 and 0.5 µM; decreases tumor volume and increases survival in a U87MG orthotopic mouse xenograft model 30 mg/kg