Home Protein Tyrosine Kinase VEGFR inhibitor - FGFR inhibitor Lucitanib (E3810) hydrochloride

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Lucitanib (E3810) hydrochloride VEGFR inhibitor

Cat.No.S7647

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 VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 479.96

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 479.96 Formula

C26H26ClN3O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1058137-23-7 -- Storage of Stock Solutions

Synonyms AL3810 Smiles [Cl-].CNC(=O)C1=CC=CC2=C1C=CC(=C2)OC3=CC=NC4=CC(=C(OC)C=C34)OCC5([NH3+])CC5

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (122.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 59 mg/mL

Ethanol : 30 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
VEGFR1 [1]
(Cell-free assay)
7 nM
VEGFR3 [1]
(Cell-free assay)
10 nM
FGFR1 [1]
(Cell-free assay)
17.5 nM
VEGFR2 [1]
(Cell-free assay)
25 nM
FGFR2 [1]
(Cell-free assay)
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04042116 Suspended
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
Advanced Cancer
Teresa Helsten MD|Clovis Oncology Inc.|University of California San Diego
 April 2017 Phase 2
NCT02202746 Terminated
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
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

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