Lucitanib (E3810) hydrochloride

Catalog No.S7647 Batch:S764701

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Technical Data

Formula

C26H26ClN3O4
Molecular Weight 479.96 CAS No. 1058137-23-7
Solubility (25°C)* In vitro DMSO 59 mg/mL (122.92 mM)
Water 59 mg/mL (122.92 mM)
Ethanol 30 mg/mL (62.5 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[1]
  • Animal Models

    Six-to eight-week-old female NCr-nu/nu mice

  • Dosages

    20 mg/kg

  • Administration

    p.o.

Selleck's Lucitanib (E3810) hydrochloride has been cited by 1 publication

Efficacy of futibatinib, an irreversible fibroblast growth factor receptor inhibitor, in FGFR-altered breast cancer [ Sci Rep, 2023, 13(1):20223] PubMed: 37980453

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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