Lucitanib

WARNING: This product is for research use only, not for human or veterinary use.

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.

Price and Availability

Lucitanib (E-3810) is not in stock, but is available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 205837Name: LucitanibCAS#: 1058137-23-7Chemical Formula: C26H25N3O4Exact Mass: 443.18451Molecular Weight: 443.4944Elemental Analysis:C, 70.41; H, 5.68; N, 9.47; O, 14.43

Synonym:E3810; E-3810; E 3810; AL3810; AL 3810; AL-3810; Lucitanib.

IUPAC/Chemical Name:6-((7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-N-methyl-1-naphthamide

InChi Key: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 Code:O=C(NC)C1=C2C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C34)=CC2=CC=C1

Technical Data

References

1: Colzani M, Noberini R, Romanenghi M, Colella G,Pasi M, Fancelli D, Varasi M, Minucci S, Bonaldi T. Quantitativechemical proteomics identifies novel targets of the anti-cancer multi-kinaseinhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. doi:10.1074/mcp.M113.034173. Epub 2014 Apr 2. PubMed PMID: 24696502; PubMedCentral PMCID: PMC4047469.

2: Zangarini M, Ceriani L, Bello E, Damia G, Cereda R, Camboni MG,Zucchetti M. HPLC-MS/MS method for quantitative determination of thenovel dual inhibitor of FGF and VEGF receptors E-3810 in tumor tissuesfrom xenograft mice and human biopsies. J Mass Spectrom. 2014Jan;49(1):19-26. doi: 10.1002/jms.3305. PubMed PMID: 24446259.

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 withpaclitaxel inhibits the growth of advanced-stage triple-negative breastcancer 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: Damia G, Colella G, Camboni G, D"Incalci M. Is PDGFR an importanttarget for E-3810? J Cell Mol Med. 2012 Nov;16(11):2838-9. doi:10.1111/j.1582-4934.2012.01601.x. PubMed PMID: 22805298.

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

6: Bello E, Colella G, Scarlato V, Oliva P, Berndt A, Valbusa G, SerraSC, D"Incalci M, Cavalletti E, Giavazzi R, Damia G, Camboni G. E-3810 isa potent dual inhibitor of VEGFR and FGFR that exerts antitumor activityin multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. PubMed PMID:21212416.

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