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Lucitanib (E3810) hydrochloride VEGFR inhibitor

Name: Lucitanib (E3810) hydrochloride
Brand: Selleck Chemicals
SKU: S7647
Rating: 5 (1 reviews)

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.

Chemical Structure

Molecular Weight: 479.96

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Quality Control

Batch: Purity: 99.58%

99.58

Related Targets	EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other VEGFR Inhibitors	SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl

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	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	VEGFR1 (Cell-free assay) 7 nM VEGFR3 (Cell-free assay) 10 nM FGFR1 (Cell-free assay) 17.5 nM VEGFR2 (Cell-free assay) 25 nM FGFR2 (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.
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).
References	[1] https://pubmed.ncbi.nlm.nih.gov/21212416/

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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