An orally bioavailable inhibitor of numerous tyrosine kinases (TKs) including fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor type 2 (VEGFR2; KDR), and colony stimulating factor 1 receptor (CSF1R; CSF-1R), with potential antiangiogenic and antineoplastic activities. Upon oral administration, simmitinib binds to and inhibits the activities of these TKs, thereby preventing both the activation of downstream signaling pathways and the proliferation of tumor cells overexpressing these TKs. FGFR, VEGFR2, and CSF1R are upregulated in a variety of cancer cell types and play key roles in tumor cell proliferation, angiogenesis, and metastasis.