Lucitanib (E3810) hydrochloride

For research use only.

Catalog No.S7647 Synonyms: AL3810

Lucitanib (E3810) hydrochloride Chemical Structure

CAS No. 1058137-23-7

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.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

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

Cell Research:

[1]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Six-to eight-week-old female NCr-nu/nu mice
  • Dosages: 20 mg/kg
  • Administration: PO
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 479.96
Formula

C26H26ClN3O4

CAS No. 1058137-23-7
Storage powder
in solvent
Synonyms AL3810

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

VEGFR Signaling Pathway Map

Related VEGFR Products

Tags: buy Lucitanib (E3810) hydrochloride | Lucitanib (E3810) hydrochloride supplier | purchase Lucitanib (E3810) hydrochloride | Lucitanib (E3810) hydrochloride cost | Lucitanib (E3810) hydrochloride manufacturer | order Lucitanib (E3810) hydrochloride | Lucitanib (E3810) hydrochloride distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID