SKLB610

SKLB610 is an inhibitor of VEGF receptor 2 (VEGFR2).¹ It inhibits VEGFR2 activity by 97% but also inhibits FGFR2 and PDGFRβ activity by 65 and 55%, respectively, when used at a concentration of 10 µM. It is selective for VEGFR2, FGFR2, and PDGFRβ over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at 10 µM. SKLB610 inhibits phosphorylation of VEGFR2 induced by VEGF in human umbilical vein endothelial cells (HUVECs). It inhibits proliferation of HUVECs induced by VEGF and basic FGF (bFGF; IC₅₀s = 2.2 and 4.7 µM, respectively). It also inhibits HUVEC capillary tube formation and migration when used at concentrations of 2.5 and 10 µM, respectively. SKLB610 inhibits proliferation of a variety of cancer cells, including A549 human lung cancer, HCT116 human colorectal carcinoma, MDA-MB-231 human mammary carcinoma, Raji human Burkitt's lymphoma, and DU145 human prostate cancer cells (IC₅₀s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM, respectively). It reduces tumor growth in A549 and HCT116 mouse xenograft models when administered at a dose of 50 mg/kg per day.

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1. Cao, Z.X., Zheng, R.L., and Lin, H.J. SKLB610: A novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol. Biochem. 27(5), 565-574 (2011).