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PDGFR&FGFR

E-3810 (1058137-23-7)

E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.

Not Intended for Therapeutic Use. For research use only.

CAS: 1058137-23-7 Category

E-3810 (1058137-23-7) Description:

Lucitanib , also known as E-3810 and AL3810, is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity. VEGFR/FGFR dual kinase inhibitor E-3810 inhibits VEGFR-1, -2, -3 and FGFR-1, -2 kinases in the nM range, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and FGFRs belong to the family of receptor tyrosine kinases that may be upregulated in various tumor cell types.

E-3810 exerted potent inhibition effects on all the three receptors of VEGFR family and two members (FGFR-1 and 2) of FGFR family in MTS assay. It also had effects on colony stimulating factor (CSF)-1R with IC50 value of 5 nM. When treated with human umbelical vein cells (HUVEC), E-3810 significantly inhibited cell proliferation induced by the addition of VEGF and bFGF with IC50 values of 40 and 50 nM, respectively. In NIH3T3 cells, E-3810 showed no inhibitory efficacy on PDGFR until the concentration of it was up to μM range, demonstrating the selectivity of E-3810.

E-3810 (1058137-23-7) Specifications:

Product Name E-3810
Synonym E3810; E-3810; E 3810; AL3810; AL 3810; AL-3810; Lucitanib.
Chemical Name 6-[7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl]oxy-N-methylnaphthalene-1-carboxamide
Purity ≥98% (HPLC)
CAS Number 1058137-23-7
Molecular Formula C26H25N3O4
Molecular Weight 443.503 g/mol
Monoisotopic Mass 443.185 g/mol
MDL number MFCD20527751
InChIKey CUDVHEFYRIWYQD-UHFFFAOYSA-N
InChi Code InChI=1S/C26H25N3O4/c1-28-25(30)19-5-3-4-16-12-17(6-7-18(16)19)33-22-8-11-29-21-14-24(23(31-2)13-20(21)22)32-15-26(27)9-10-26/h3-8,11-14H,9-10,15,27H2,1-2H3,(H,28,30)
SMILES O=C(NC)C1=C2C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C34)=CC2=CC=C1
Form Powder
Color N/A
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application a potent and selective dual inhibitor of VEGF and FGF receptors

 


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RIDADR NONH for all modes of transport

References:

[1]. Kawai T, Ikeda H, Harada Y, Saitou T. [Changes in the rat stomach after long-term administration of proton pump inhibitors (AG-1749 and E-3810)]. Nihon Rinsho. 1992 Jan;50(1):188-93. Japanese. PubMed PMID: 1311785.

[2]. Colzani M, Noberini R, Romanenghi M, Colella G, Pasi M, Fancelli D, Varasi M, Minucci S, Bonaldi T. 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. Epub 2014 Apr 2. PubMed PMID: 24696502; PubMed Central PMCID: PMC4047469.

[3]. Bello E, Taraboletti G, Colella G, Zucchetti M, Forestieri D, Licandro SA, Berndt A, Richter P, D’Incalci M, Cavalletti E, Giavazzi R, Camboni G, Damia G. 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. doi: 10.1158/1535-7163.MCT-12-0275-T. Epub 2012 Dec 27. PubMed PMID: 23270924.

[4]. Sala F, Bagnati R, Livi V, Cereda R, D’Incalci M, Zucchetti M. Development and validation of a high-performance liquid chromatography-tandem mass spectrometry method for the determination of the novel inhibitor of angiogenesis E-3810 in human plasma and its application in a clinical pharmacokinetic study. J Mass Spectrom. 2011 Oct;46(10):1039-45. doi: 10.1002/jms.1985. PubMed PMID: 22012670.

[5]. Synergistic anti-angiogenic treatment effects by dual FGFR1 and VEGFR1 inhibition in FGFR1-amplified breast cancer Publication name:Oncogene PMID: 29970903

1 review for E-3810 (1058137-23-7)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The E-3810 (1058137-23-7) is high purity,also customer service is pretty nice !gotta try!!

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