Lucitanib (E3810)

Description: Lucitanib (formerly also known as E3810 and AL3810; E-3810) is a novel and potent dual inhibitor of human vascular endothelial growth factor receptors VEGFR and FGFR, it potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. Lucitanib inhibits VEGFR-1, -2, -3 and FGFR-1, -2 kinases in the nM range, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and FGFRs belong to the family of receptor tyrosine kinases that may be upregulated in various tumor cell types.

References: Cancer Res. 2011 Feb 15; 71(4):1396-405.; Mol Cell Proteomics. 2014 Jun; 13(6):1495-509.