| Identification | Back Directory | [Name]
1-Naphthalenecarboxamide, 6-[[7-[(1-aminocyclopropyl)methoxy]-6-methoxy-4-quinolinyl]oxy]-N-methyl-, hydrochloride (1:2) | [CAS]
2108875-91-6 | [Synonyms]
1-Naphthalenecarboxamide, 6-[[7-[(1-aminocyclopropyl)methoxy]-6-methoxy-4-quinolinyl]oxy]-N-methyl-, hydrochloride (1:2) | [Molecular Formula]
C26H26ClN3O4 | [MOL File]
2108875-91-6.mol | [Molecular Weight]
479.96 |
| Hazard Information | Back Directory | [Uses]
Lucitanib (E-3810) dihydrochloride is a novel dual inhibitor of VEGFR and FGFR, 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[1][2][3]. | [in vivo]
Lucitanib (E-3810), at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. Lucitanib (E-3810) shows a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas) with dose-dependent inhibition of tumor growth. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment is suspended; in a few cases, tumor regression is observed[1]. The activity of Lucitanib (E-3810) given at the doses of 15 mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib (E-3810), with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib (E-3810) at a rate similar to control tumors[3]. | [IC 50]
VEGFR1: 7 nM (IC50); VEGFR2: 25 nM (IC50); VEGFR3: 10 nM (IC50); FGFR1: 17.5 nM (IC50); FGFR2: 82.5 nM (IC50) | [References]
[1] Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. DOI:10.1158/0008-5472.CAN-10-2700
[2] Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. DOI:10.1074/mcp.M113.034173
[3] Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with NSC 125973 inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40 DOI:10.1158/1535-7163.MCT-12-0275-T |
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