For research use only. Not for therapeutic Use.
First-in-class dual VEGFR/FGFR tyrosine kinase inhibitor; E-3810 potently and selectively inhibited VEGFR1, -2, and -3 and FGFR-1 and -2 kinases in the nanomolar range; a potent antiangiogenic small molecule with a favorable pharmacokinetic profile and broad spectrum antitumor activity
| Catalog Number | I047578 |
| CAS Number | 2108875-91-6 |
| Molecular Formula | C26H25N3O4.2HCl |
| Purity | ≥95% |
| IUPAC Name | 6-[7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl]oxy-N-methylnaphthalene-1-carboxamide;dihydrochloride |
| InChI | InChI=1S/C26H25N3O4.2ClH/c1-28-25(30)19-5-3-4-16-12-17(6-7-18(16)19)33-22-8-11-29-21-14-24(23(31-2)13-20(21)22)32-15-26(27)9-10-26;;/h3-8,11-14H,9-10,15,27H2,1-2H3,(H,28,30);2*1H |
| SMILES | CNC(=O)C1=CC=CC2=C1C=CC(=C2)OC3=C4C=C(C(=CC4=NC=C3)OCC5(CC5)N)OC.Cl.Cl |
| Reference | E Bello et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011, 71(4), 1396-1405.
JC Soria et al. First-in-man study of E-3810, a novel VEGFR and FGFR inhibitor, in patients with advanced solid tumors. Ann. Oncol. 2011, 22, 40.
Y Zhou et al. AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR. J. Cell Mol. Med. 2012, 16(10), 2321-2330.
G Damia et al. Is PDGFR an important target for E-3810? J. Cell Mol. Med. 2012, 16(11), 2838-2839. [Letter to the Editor] |
