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Lucitanib

Catalog No. T15185   CAS 1058137-23-7
Synonyms: E-3810

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).

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Lucitanib Chemical Structure
Lucitanib, CAS 1058137-23-7
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
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Purity: 96.13%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (56.37 mM)

TargetMolReferences and Literature

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. 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. 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

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library NO PAINS Compound Library Anti-Liver Cancer Compound Library Cytokine Inhibitor Library Inhibitor Library Anti-Ovarian Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library

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Keywords

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

 

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