SKLB610 is a VEGFR inhibitor that potently suppresses human tumor angiogenesis. SKLB610 inhibits angiogenesis-related tyrosine kinase VEGFR2, fibroblast growth factor receptor 2 (FGFR2) and platelet-derived growth factor receptor (PDGFR) at rate of 97%, 65% and 55%, respectively, at concentration of 10 μM in biochemical kinase assays.SKLB610 exhibits its antitumor activity as a multi-targeted inhibitor with more potent inhibition of VEGFR2 activity.