Lucitanib

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

MedKoo CAT#: 205837

CAS#: 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.


Price and Availability

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Price

10mg
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100mg
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1g
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Size
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25mg
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200mg
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2g
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Size
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50mg
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500mg
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5g
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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

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Theoretical Analysis

MedKoo Cat#: 205837
Name: Lucitanib
CAS#: 1058137-23-7
Chemical Formula: C26H25N3O4
Exact Mass: 443.18451
Molecular Weight: 443.4944
Elemental 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

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: 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.

2: Zangarini M, Ceriani L, Bello E, Damia G, Cereda R, Camboni MG, Zucchetti M. 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. J Mass Spectrom. 2014 Jan;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 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: Damia G, Colella G, Camboni G, D'Incalci M. Is PDGFR an important target 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 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.

6: 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. 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. 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 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.