E-3810 is a small-molecule dual inhibitor of VEGF and FGF receptors with IC 50 values of 7, 25, 10, 17.5, 82.5 and 237.5 nM for VEGFR-1, 2, 3, FGFR-1, 2 and 3, respectively [1]. The vascular endothelial growthfactor (VEGF) and fibroblast growth factor (FGF) are important factors in angiogenesis. They promote the process of angiogenesis through binding to their associated tyrosine kinase receptors and trigger a cascade signaling pathway that finally leads to the increased proliferation of the blood vessel cells and permeability of the vessels. Tumor cells are rapidly proliferating cells which need more vessels to deliver nutrients, therefore VEGFR and FGFR are attractive targets in antitumor treatment. As a selective inhibitor of VEGFR and FGFR, E-3810 shows potent effects in both in vitro and in vivo assays [1]. E-3810 exerted potent inhibition effects on all the three receptors of VEGFR family and two members (FGFR-1 and 2) of FGFR family in MTS assay. It also had effects on colony stimulating factor (CSF)-1R with IC50 value of 5 nM. When treated with human umbelical vein cells (HUVEC), E-3810 significantly inhibited cell proliferation induced by the addition of VEGF and bFGF with IC50 values of 40 and 50 nM, respectively. In NIH3T3 cells, E-3810 showed no inhibitory efficacy on PDGFR until the concentration of it was up to μM range, demonstrating the selectivity of E-3810 [1]. In the mice model, oral administration of 20 mg/kg E-3810 for 7 days significantly inhibited vessel formation induced by bFGF. E-3810 also exerted effective inhibition on tumor growth in variety of human tumor xenografts such as A498, HT29 and A2780. Besides that, it was reported that the combination treatment of E-3810 and paclitaxel showed higher antitumor activity than that of paclitaxel with brivanib or sunitinib in the MDA-MB-231 breast cancer xenografts [1, 2]. References: [1]. Bello E, Colella G, Scarlato V, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer research, 2011, 71(4): 1396-1405. [2]. Bello E, Taraboletti G, Colella G, et al. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Molecular cancer therapeutics, 2013, 12(2): 131-140.
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Biological Activity
Description
E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
