Home Protein Tyrosine Kinase VEGFR inhibitor - FGFR inhibitor Lucitanib (E3810) hydrochloride For research use only.

Lucitanib (E3810) hydrochloride

Synonyms: AL3810

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

Lucitanib (E3810) hydrochloride Chemical Structure

CAS No. 1058137-23-7

Purity & Quality Control

Lucitanib (E3810) hydrochloride Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

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

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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Six-to eight-week-old female NCr-nu/nu mice
Dosages 20 mg/kg
Administration p.o.
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

Chemical Information & Solubility

Molecular Weight 479.96 Formula

C26H26ClN3O4
CAS No. 1058137-23-7 SDF --
Smiles [Cl-].CNC(=O)C1=CC=CC2=C1C=CC(=C2)OC3=CC=NC4=CC(=C(OC)C=C34)OCC5([NH3+])CC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 59 mg/mL ( (122.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 59 mg/mL

Ethanol : 30 mg/mL


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In vivo
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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.

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