Home Protein Tyrosine Kinase VEGFR inhibitor - FGFR inhibitor - PDGFR inhibitor - c-Kit inhibitor - c-RET inhibitor Lenvatinib Mesylate For research use only.

Lenvatinib Mesylate

Synonyms: E7080 mesylate

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.

Lenvatinib Mesylate Chemical Structure

Lenvatinib Mesylate Chemical Structure

CAS No. 857890-39-2

Purity & Quality Control

Lenvatinib Mesylate Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Click to View More Cell Line Experimental Data

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)		 Click to View More Targets
4.0 nM 5.2 nM 22 nM 39 nM
In vitro
In vitro

E7080 is an orally active inhibitor of multiple receptor tyrosine kinases including VEGF, FGF and SCF receptors.
Experimental Result Images Methods Biomarkers Images PMID
Western blot phospho-FGFR1 / FGFR1 /phospho-FRS2 / FRS2 / phospho-MEK / phospho-ERK phospho-RET / phospho-ERK Ki-67 / Cyclin D1 / CDK4 / p21 / p53 / Apaf-1 / p-NFκB / Bcl-2 / Cleaved-caspase 3 Vimentin / E-cadherin / Snail / Zeb1 25295214
Growth inhibition assay Cell viability 25425971
Immunofluorescence β-catenin 30286728
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06161558 Not yet recruiting
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 1
NCT05846724 Not yet recruiting
Kaposi Sarcoma|Classic Kaposi Sarcoma|Refractory Kaposi Sarcoma
Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico
 February 1 2024 Phase 2
NCT05903833 Not yet recruiting
Recurrent Vulvar Cancer|Persistent Vulvar Cancer|Metastatic Vulva Cancer|Locally Advanced Vulvar Cancer
AGO Research GmbH
 January 1 2024 Phase 2
NCT05901194 Not yet recruiting
Hepatocellular Carcinoma Non-resectable
Assistance Publique - Hôpitaux de Paris|Laboratoire EISAI
 June 2023 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 522.96 Formula

C21H19ClN4O4.CH4O3S
CAS No. 857890-39-2 SDF --
Smiles COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl.CS(=O)(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 39 mg/mL ( (74.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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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.

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