E-3810 | CAS:1058137-23-7

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Name:E-3810; Lucitanib
Cat. No. :CS-0782
CAS No. :1058137-23-7
Formula:C26H25N3O4
M. Wt. : 443.49
Solubility:10 mM in DMSO

E-3810 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.IC50 & Target: IC50: 7 nM (VEGFR1), 25 nM (VEGFR2), 10 nM (VEGFR3), 17.5 nM (FGFR1), 82.5 nM (FGFR2), 5 nM (CSF-1R)[1]In Vitro: Consistent with the inhibitory activity of VEGFR and FGFR auto-phosphorylation, E-3810 potently inhibits VEGF and bFGF-stimulated HUVEC proliferation with IC50 of 40 and 50 nM, respectively. Besides, E-3810 also inhibits CSF-1R with IC50 of 5 nM[1]. E-3810 potently inhibits FGFR2 activity (Kii=0.11 μM). The Ki values obtained for DDR2, LYN, CARDIAK, CSBP (2), EPHA2, and YES range between 0.26 and 8 μM[2]. In Vivo: E-3810, at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P[1]. The activity of 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 E-3810, with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of E-3810 at a rate similar to control tumors[3].

Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40. 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. 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.