lenvatinib Mesylate

For research use only.

Catalog No.S5240

10 publications

lenvatinib Mesylate Chemical Structure

CAS No. 857890-39-2

Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.

Size Price Stock Quantity  
USD 97 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's lenvatinib Mesylate has been cited by 10 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.
Targets
c-RET [2]
()
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
4.0 nM 5.2 nM 22 nM 39 nM
Assay
Methods Test Index PMID
Western blot
phospho-FGFR1 / FGFR1 /phospho-FRS2 / FRS2 / phospho-MEK / phospho-ERK ; 

PubMed: 25295214     


Effect of lenvatinib on FGFR1 signaling pathway in human DTC RO82-W-1 cells in vitro. After starvation overnight, RO82-W-1 cells were treated with vehicle (control), lenvatinib or sorafenib at the indicated concentrations for 1 h and were then stimulated for 10 min with bFGF (20 ng/mL) and heparin before being lysed. Western blot analyses of the phosphorylation of FGFR1 and its downstream effectors in RO82-W-1 cells were then performed and representative images were shown.

phospho-RET / phospho-ERK; 

PubMed: 25295214     


Western blot analyses of the phosphorylation of RET in human medullary thyroid TT cells. TT cells were seeded and cultured overnight. They were then treated with lenvatinib at the indicated concentrations for 1 h before being lysed.

Ki-67 / Cyclin D1 / CDK4 / p21 / p53 / Apaf-1 / p-NFκB / Bcl-2 / Cleaved-caspase 3; 

PubMed: 30286728     


Immunoblot analysis of cell-cycle arrest and apoptotic proteins showed marked increase in the levels of p21, p53, Apaf-1, and cleaved caspase 3, and decrease in the levels of Ki-67, cyclin D1, CDK 4, p-NFkB, and Bcl-2 in the SoLAT group than in the individual sorafenib or lenvatinib treatment groups.

Vimentin / E-cadherin / Snail / Zeb1 ; 

PubMed: 30286728     


(b and d) Immunoblot analysis of EMT markers showed that most EMT markers such as vimentin, E-cadherin, Snail, and Zeb1 were inhibited by FGFR inhibition (p-ERK1/2) in the SoLAT group.

25295214 30286728
Growth inhibition assay
Cell viability; 

PubMed: 25425971     


Dose-response effects of E7080 on cell viability of human colorectal carcinoma (CRC) cells and endothelial cells (HUVEC). IC50 values were determined in serum reduced (1%) RPMI 1640 medium following treatment with different concentrations of E7080 for 72 hours. The final concentration of DMSO (vehicle) was ≤1%. Results are expressed as the mean ± S.E.M. of at least three independent proliferation assays with hexaplicates.

25425971
Immunofluorescence
β-catenin; 

PubMed: 30286728     


(a and c) Immunofluorescence assay for nuclear translocation of β-catenin. Results confirmed that SoLAT inhibited nuclear translocation of β-catenin in the advanced PTC cells more potently than either agent alone.

30286728

Protocol

Solubility (25°C)

In vitro DMSO 39 mg/mL (74.57 mM)
Ethanol '-1 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 522.96
Formula

C21H19ClN4O4.CH4O3S

CAS No. 857890-39-2
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl.CS(=O)(=O)O

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 MSDS / 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 MSDS / 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
NCT04519151 Not yet recruiting Drug: Pembrolizumab|Drug: Lenvatinib Ovarian Neoplasms|Carcinoma Ovarian Epithelial|Neoplasm of Stomach|Ovarian Diseases|Genital Neoplasms Female|Ovarian Epithelial Tumor|Urogenital Neoplasms|Neoplasms Glandular and Epithelial Sheba Medical Center November 2020 Phase 2
NCT04447755 Recruiting Drug: Lenvatinib Relapsed or Refractory Solid Tumors Merck Sharp & Dohme Corp.|Eisai Inc. July 30 2020 Phase 2
NCT04287829 Not yet recruiting Drug: Pembrolizumab|Drug: Lenvatinib Mesotheliomas Pleural The Netherlands Cancer Institute|Merck Sharp & Dohme Corp. May 5 2020 Phase 2
NCT04154189 Recruiting Drug: Lenvatinib|Drug: Ifosfamide|Drug: Etoposide Osteosarcoma Eisai Inc.|Merck Sharp & Dohme Corp. March 23 2020 Phase 2
NCT04042805 Not yet recruiting Biological: Sintilimab|Drug: Lenvatinib Hepatocellular Carcinoma Baocai Xing|Beijing Cancer Hospital August 1 2019 Phase 2
NCT03732495 Recruiting Drug: Lenvatinib + Denosumab Thyroid Cancer Metastatic Centre Leon Berard July 26 2019 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 lenvatinib Mesylate | lenvatinib Mesylate supplier | purchase lenvatinib Mesylate | lenvatinib Mesylate cost | lenvatinib Mesylate manufacturer | order lenvatinib Mesylate | lenvatinib Mesylate distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID