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SKLB1002 showed potent inhibition of VEGFR2 kinase activity (IC50 = 32 nmol/L), which was similar with the positive drugs vandetanib (IC50 = 40 nmol/L) and sunitinib (IC50 = 9 nmol/L). SKLB1002 significantly inhibited endothelial cell proliferation with an IC50 value of 11.9 μmol/L. However, vandetanib and sunitinib inhibited cell viability at a much lower concentration with an IC50 value of 3.8 μmol/L and 1.9 μmol/L, respectively .