Description

Product Description

Lenvatinib Mesilate (CAS 857890-39-2) is a highly potent, orally active, multi-targeted tyrosine kinase inhibitor (TKI) that has gained prominence in preclinical oncology research due to its broad-spectrum activity against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT. These receptor tyrosine kinases play critical roles in tumor angiogenesis, proliferation, survival, and metastasis. The compound’s solution formulation allows precise dosing in both in vitro and in vivo studies, facilitating mechanistic investigations and pharmacodynamic analyses.

Chemical and Structural Features

Lenvatinib Mesilate is the mesilate salt form of Lenvatinib, a small molecule with a molecular formula of C21H19ClN4O4·CH4O3S and a molecular weight of 426.32 g/mol (free base). The chemical structure consists of a pyrimidine core linked to multiple aromatic and heterocyclic moieties, which confer high affinity for ATP-binding sites on target kinases. This structure allows selective inhibition of VEGFR, FGFR, PDGFR, RET, and KIT kinases, thereby modulating critical signaling pathways in endothelial and tumor cells.

The solution form is typically prepared in DMSO, ethanol, or water-based buffers and can be adjusted between 1–10 mM for experimental needs. Stability studies indicate that the solution is stable under refrigeration (2–8 °C) and should be protected from light to maintain its biological activity. Repeated freeze-thaw cycles should be avoided to prevent degradation.

Pharmacological Significance

Lenvatinib Mesilate demonstrates significant inhibitory activity against key receptor tyrosine kinases involved in angiogenesis and tumor progression:

• VEGFR1–3: Lenvatinib blocks VEGF-mediated signaling, preventing endothelial cell proliferation, migration, and tube formation.

• FGFR1–4: By inhibiting FGF-driven signaling, it affects tumor microenvironment remodeling, angiogenic sprouting, and contributes to overcoming resistance mechanisms in tumors.

• PDGFRα, RET, KIT: These targets are critical in tumor proliferation, survival, and migration. Lenvatinib’s inhibition reduces tumor growth and metastasis potential.

The multi-targeted profile makes Lenvatinib Mesilate a versatile tool for preclinical oncology studies, enabling researchers to dissect the complex signaling networks regulating angiogenesis, proliferation, and apoptosis in cancer models. It has been applied extensively in endothelial cell assays, tumor spheroid models, xenograft studies, and mechanistic in vitro experiments.

Preclinical Applications

Lenvatinib Mesilate solution is particularly suitable for:

• Angiogenesis Studies: Investigating VEGFR- and FGFR-mediated pathways in endothelial cells, measuring tube formation, migration, and microvessel density in vitro and in vivo.

• Cancer Cell Proliferation Assays: Assessing cell viability, proliferation, and apoptosis in multiple tumor cell lines, including hepatocellular carcinoma, thyroid cancer, and renal cell carcinoma models.

• Combination Therapy Research: Evaluating synergistic or antagonistic effects with chemotherapeutics, other kinase inhibitors, immunotherapies, or radiation treatment.

• Resistance Mechanism Studies: Studying acquired resistance mechanisms, including upregulation of alternative RTKs, mutations in VEGFR/FGFR, and downstream PI3K/AKT or MAPK/ERK signaling adaptations.

• Signal Transduction Investigations: Elucidating downstream pathways modulated by VEGFR/FGFR/PDGFR/RET/KIT, including PI3K/AKT, MAPK/ERK, PLCγ, STAT, and NF-κB pathways.

This extensive utility makes Lenvatinib Mesilate solution an indispensable reagent in oncology research and angiogenesis studies.

Product Specifications

Lenvatinib Mesilate Mechanism of Action

Multi-Kinase Inhibition

Lenvatinib Mesilate acts primarily by binding to the ATP-binding sites of multiple receptor tyrosine kinases: VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT. By preventing phosphorylation of these kinases, downstream signaling cascades such as PI3K/AKT, MAPK/ERK, PLCγ, STAT, and NF-κB are suppressed, leading to:

• Reduced endothelial proliferation and tube formation

• Inhibition of tumor cell growth and survival

• Induction of apoptotic pathways

• Suppression of angiogenesis and metastasis

Apoptosis Induction

• Mitochondrial depolarization and cytochrome c release

• Activation of caspase-3 and caspase-9, engaging intrinsic apoptotic pathways

• ROS generation contributing to oxidative stress

• Crosstalk with p53-dependent and independent pathways

Preclinical Research Applications

• Angiogenesis Studies: Lenvatinib reduces microvessel density and endothelial cell migration in vitro and in vivo.

• Combination Therapy Evaluation: Can be combined with chemotherapeutic agents, immunotherapies, or other TKIs to evaluate synergistic or antagonistic effects.

• Resistance Mechanism Research: Used to study VEGFR/FGFR pathway adaptations, compensatory signaling, and kinase mutations in tumor models.

• Signal Transduction Analysis: Facilitates mapping of downstream effectors in PI3K/AKT, MAPK/ERK, PLCγ, STAT, and NF-κB pathways.

  

Lenvatinib Mesilate Side Effects (Preclinical Observations)

Cellular Effects

• Reduced endothelial cell proliferation and tube formation

• Suppressed tumor cell migration and invasion

• Modulation of intracellular calcium signaling and stress-response pathways

• ROS-mediated oxidative stress and DNA damage

Apoptotic Effects

• Caspase-dependent apoptosis in tumor and endothelial cells

• Mitochondrial membrane depolarization and intrinsic pathway activation

• p53-dependent and independent apoptotic signaling

Laboratory Handling

• Use appropriate PPE and work in a fume hood

• Store solution at 2–8 °C and protect from light

• Avoid repeated freeze-thaw cycles

Follow institutional biosafety and chemical handling protocols

Keywords

Lenvatinib Mesilate, E7080 Mesilate, multi-kinase inhibitor, VEGFR inhibitor, FGFR inhibitor, PDGFR inhibitor, RET inhibitor, KIT inhibitor, angiogenesis research, apoptosis studies, cytotoxicity assays, preclinical oncology, high-purity research chemical, factory small-molecule supplier, China chemical manufacturer, OEM & bulk production, laboratory research reagent

Shipping Guarantee

All Lenvatinib Mesilate shipments of Lenvatinib Mesilate solution are handled using validated cold-chain logistics to ensure compound integrity. Packages are sealed with secondary protective wrapping and shipped via express international couriers with full tracking and insurance. Shipment conditions are monitored to maintain solution stability and bioactivity during transit.

Trade Assurance

We Lenvatinib Mesilate guarantee the authenticity and quality of all Lenvatinib Mesilate batches. Purity is verified at ≥99% using HPLC, MS, and NMR. Certificates of Analysis (CoA) are provided for each batch. Replacement or refund is assured for any deviation from listed specifications.

Payment Support

Lenvatinib Mesilate Flexible global payment options are available:

• PayPal

• Major credit cards (Visa, MasterCard, American Express)

• Bank transfer (T/T)

• Cryptocurrencies (USDT, Bitcoin, Ethereum)

All Lenvatinib Mesilate transactions are encrypted and verified to ensure confidentiality and security.

Disclaimer

Lenvatinib Mesilate is strictly for laboratory research purposes. Not for human or veterinary use. Researchers must adhere to institutional safety and chemical handling protocols. Supplier assumes no liability for misuse.

References

• PubChem: Lenvatinib Mesilate (CID 135398842)

• ChEMBL: Lenvatinib Bioactivity Summary (CHEMBL2087753)

• DrugBank: Lenvatinib – DB09091

• PubMed: Lenvatinib Mechanism and Preclinical Studies (PMID 28837672)

• IUPHAR/BPS Guide to Pharmacology: VEGFR Inhibitors