Lucitanib (E3810) hydrochloride

Catalog No.S7647 Synonyms: AL3810

For research use only.

Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

Lucitanib (E3810) hydrochloride Chemical Structure

CAS No. 1058137-23-7

Purity & Quality Control

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Biological Activity

Description Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
Targets
VEGFR1 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
7 nM 10 nM 17.5 nM 25 nM 82.5 nM
In vitro

In vitro Lucitanib (E3810) inhibits the VEGF- and bFGF-dependent proliferation and the signaling transduction pathways elicited by VEGF and bFGF ligands binding to their cognate receptors in HUVEC cells in the nanomolar range.[1]

In vivo

In vivo 7 days of treatment with Lucitanib (E3810) completely inhibites the FGF-induced angiogenesis in an implanted Matrigel plug in mice; Lucitanib (E3810) treatment significantly reduces tumor vessel density in treated tumors (as assessed by the decrease in CD31 staining), increasing in the percentage of tumor necrosis and changing the composition of tumor stroma (with a decrease in collagen IV content).[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HUVEC cells, NHI3T3 cells
  • Concentrations: 10 mM
  • Incubation Time: 72 h
  • Method:

    Exponentially growing HUVEC or NHI3T3 cells are seeded into 96-well plates at a density of 3 to 6×103 cells/100 μL/well in complete medium. In the experiments without serum starvation, 24 hours after seeding, cells are exposed to different Lucitanib (E3810) concentrations without or with VEGF165(50 ng/mL) or bFGF (20 ng/mL) ligands and the antiproliferative effect of the drugs is evaluated after 72 hours by MTS Colorimetric Assay.

Animal Research:

[1]

  • Animal Models: Six-to eight-week-old female NCr-nu/nu mice
  • Dosages: 20 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 59 mg/mL
(122.92 mM)
Water 59 mg/mL
(122.92 mM)
Ethanol '''30 mg/mL

Chemical Information

Molecular Weight 479.96
Formula

C26H26ClN3O4

CAS No. 1058137-23-7
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04042116 Recruiting Drug: Lucitanib|Drug: Nivolumab Advanced Solid Tumor|Gynecologic Cancer Clovis Oncology Inc.|Bristol-Myers Squibb|European Network of Gynaecological Oncological Trial Groups (ENGOT) July 29 2019 Phase 1|Phase 2
NCT02747797 Withdrawn Drug: Lucitanib Advanced Cancer Teresa Helsten MD|Clovis Oncology Inc.|University of California San Diego April 2017 Phase 2
NCT02202746 Terminated Drug: Lucitanib Breast Cancer|Metastatic Breast Cancer|MBC|HER2 Positive|HER2|Estrogen Receptor Positive|ER|Triple Negative Clovis Oncology Inc. September 9 2014 Phase 2
NCT02109016 Terminated Drug: Lucitanib Non-Small Cell Lung Cancer|Squamous Non-Small Cell Lung Cancer|NSCLC|Small Cell Lung Cancer|SCLC|Lung Cancer|Advanced Lung Cancer|Metastatic Lung Cancer|Stage IV Lung Cancer Clovis Oncology Inc. April 2014 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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