Semaxinib

Description: Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 µM), exhibiting a 20-fold greater selectivity for VEGFR2 over PDGFRbeta, with no activity against InsR, EGFR, and FGFR. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature. Target: VEGFR. Smiles: C(=C1C=2C(NC1=O)=CC=CC2)C=3NC(C)=CC3C. References: Fong TA, et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res, 1999, 59(1), 99-106.