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E-3810 CAS: 1058137-23-7

Category: Inhibitors
Product Name: E-3810
Cat No: I000297
CAS No: 1058137-23-7
Synonyms: 6-[7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl]oxy-N-methylnaphthalene-1-carboxamide
Molecular Formula: C26H25N3O4
Molecular Weight: 443.49
SMILES: O=C(NC)C1=C2C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C34)=CC2=CC=C1
InChI: None
InChIKey: None
Solubility: 10 mM in DMSO
Target: FGFR
Storage: Store at -20°C
CAS 1058137-23-7,E-3810
  • Description

E-3810 is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity.
IC50 value:
Target: VEGFR/FGFR
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.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Colzani M, Noberini R, Romanenghi M, Colella G, Pasi M, Fancelli D, Varasi M, Minucci S, Bonaldi T.Mol Cell Proteomics. 2014 Jun;13(6):1495-509. doi: 10.1074/mcp.M113.034173. Epub 2014 Apr 2. PMID: 24696502 Free PMC Article
2:HPLC-MS/MS method for quantitative determination of the novel dual inhibitor of FGF and VEGF receptors E-3810 in tumor tissues from xenograft mice and human biopsies. Zangarini M, Ceriani L, Bello E, Damia G, Cereda R, Camboni MG, Zucchetti M.J Mass Spectrom. 2014 Jan;49(1):19-26. doi: 10.1002/jms.3305. PMID: 24446259
3:The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. 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.Mol Cancer Ther. 2013 Feb;12(2):131-40. doi: 10.1158/1535-7163.MCT-12-0275-T. Epub 2012 Dec 27. PMID: 23270924 Free Article
4:Is PDGFR an important target for E-3810? Damia G, Colella G, Camboni G, D'Incalci M.J Cell Mol Med. 2012 Nov;16(11):2838-9. doi: 10.1111/j.1582-4934.2012.01601.x. No abstract available. PMID: 22805298 Free PMC Article
5: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. Sala F, Bagnati R, Livi V, Cereda R, D'Incalci M, Zucchetti M.J Mass Spectrom. 2011 Oct;46(10):1039-45. doi: 10.1002/jms.1985. PMID: 22012670
6:E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Bello E, Colella G, Scarlato V, Oliva P, Berndt A, Valbusa G, Serra SC, D'Incalci M, Cavalletti E, Giavazzi R, Damia G, Camboni G.Cancer Res. 2011 Feb 15;71(4):1396-405. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. PMID: 21212416 Free Article
7:[Changes in the rat stomach after long-term administration of proton pump inhibitors (AG-1749 and E-3810)]. Kawai T, Ikeda H, Harada Y, Saitou T.Nihon Rinsho. 1992 Jan;50(1):188-93. Japanese. PMID: 1311785


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