Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lucitanib (E-3810) is a novel VEGFR and FGFR inhibitor. It potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 (IC50s: 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 40.00 | |
2 mg | In stock | $ 57.00 | |
5 mg | In stock | $ 89.00 | |
10 mg | In stock | $ 147.00 | |
25 mg | In stock | $ 283.00 | |
50 mg | In stock | $ 513.00 | |
100 mg | In stock | $ 747.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 97.00 |
Description | Lucitanib (E-3810) is a novel VEGFR and FGFR inhibitor. It potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 (IC50s: 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively). |
Targets&IC50 | FGFR1:17.5 nM, FGFR2:82.5 nM, VEGFR1:7 nM, VEGFR3:10 nM, VEGFR2:25 nM |
In vitro | Lucitanib potently inhibits FGFR2 activity (Ki<0.05 μM), follows by PDGFRα activity (Ki=0.11 μM) and it also potently inhibits VEGF and bFGF-stimulated HUVEC proliferation (IC50: 40 and 50 nM, respectively), which consistent with the inhibitory activity of VEGFR and FGFR auto-phosphorylation. Lucitanib (E-3810) also inhibits CSF-1R (IC50: 5 nM)[1].The Ki values obtained for DDR2, LYN, CARDIAK, CSBP (2), EPHA2, and YES range between 0.26 and 8 μM[2]. |
In vivo | Lucitanib (20 mg/kg; 7 consecutive days; p.o.) treatment, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. 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 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 , with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib at a rate similar to control tumors[3]. Lucitanib displays a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas). It has dose-dependent inhibition of tumor growth. |
Synonyms | E-3810 |
Molecular Weight | 443.49 |
Formula | C26H25N3O4 |
CAS No. | 1058137-23-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (56.37 mM)
You can also refer to dose conversion for different animals. More
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Lucitanib 1058137-23-7 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR Fibroblast growth factor receptor E-3810 E 3810 Vascular endothelial growth factor receptor Inhibitor E3810 inhibit inhibitor