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Angiogenesis VEGFR Lucitanib

Lucitanib

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

Lucitanib 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).

Lucitanib, CAS 1058137-23-7
Pack Size Availability Price/USD Quantity
2 mg In stock 112.00
5 mg In stock 190.00
10 mg In stock 308.00
25 mg In stock 458.00
50 mg In stock 864.00
100 mg In stock 1296.00
200 mg In stock 1944.00
1 mL * 10 mM (in DMSO) In stock 202.00
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Purity 96.13%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Lucitanib 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 VEGFR1 : ic50 7 nM ,   VEGFR2 : ic50 25 nM ,   VEGFR3 : ic50 10 nM ,   FGFR1 : ic50 17.5 nM ,   FGFR2 : ic50 82.5 nM
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
Purity 96.13%
Molecular Weight 443.49
Formula C26H25N3O4
CAS No. 1058137-23-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 25 mg/mL (56.37 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References 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

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