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Description: SKLB610 is a novel multi-targeted kinase inhibitor with more potent inhibition of VEGFR2. It has potential anticancer activity by potently suppressing human tumor angiogenesis. It 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 10uM in biochemical kinase assays. In HUVECs, SKLB610 blocks VEGF stimulated phosphorylation of VEGFR2 in a dose dependent manner after SKLB610 treatment. SKLB610 significant inhibits HUVECs capillary tube formation in a concentration-dependent manner. Its potential to be a candidate of anticancer agent is worth being further investigated.
References: Cell Physiol Biochem. 2011; 27(5):565-74.
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