E-3810 (1058137-23-7) Description:
Lucitanib , also known as E-3810 and AL3810, is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity. VEGFR/FGFR dual kinase inhibitor E-3810 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.
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.
E-3810 (1058137-23-7) Specifications:
|Synonym||E3810; E-3810; E 3810; AL3810; AL 3810; AL-3810; Lucitanib.|
|Molecular Weight||443.503 g/mol|
|Monoisotopic Mass||443.185 g/mol|
|Solubility||Soluble in DMSO, not in water|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and moisture|
|Application||a potent and selective dual inhibitor of VEGF and FGF receptors|