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Lenvatinib

Cat. No. M1841

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Lenvatinib Structure
Synonym:

E7080

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
50mg USD 130  USD130 In stock
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Quality Control & Documentation
Biological Activity

Lenvatinib (E7080) is an orally active inhibitor of multiple receptor tyrosine kinases including VEGF, FGF and SCF receptors. Lenvatinib (E7080) has IC50s of 4, 5.2, 22 nM for VEGFR2 (KDR), VEGFR3 (Flt-4), and VEGFR1 (Flt-1), respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC50s of 51, 39, 46, and 100 nM, respectively. Lenvatinib was found to be transformed to a GSH conjugate, through displacement of an O-aryl moiety, at the quinoline part of the molecule in the liver and kidneys. The GSH conjugate underwent further hydrolysis by γ-glutamyltranspeptidase and dipeptidases, followed by intramolecular rearrangement, to form N-cysteinyl quinoline derivatives, which were dimerized to form disulfide dimers and also formed an N,S-cysteinyl diquinoline derivative.

Oral administration of Lenvatinib inhibited tumor growth of H146 cells at doses of 30 and 100 mg/kg in a dose-dependent manner and caused tumor regression at 100 mg/kg. While anti-VEGF antibody also slowed tumor growth, it did not cause tumor regression. These results indicate that KIT signaling has a role in tumor angiogenesis of SCF-producing H146 cells, and Lenvatinib causes regression of H146 tumors as a result of antiangiogenic activity mediated by inhibition of both KIT and VEGF receptor signaling.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines H146 cells
Preparation method Proliferation assay
H146 (1.2 3 103 cells/50 lL/well) in SFM containing 0.5% BSA were cultured in 96-well multi-plates. After overnight culture at 37℃, SFM (150 lL/well) containing 0.5% FBS and several concentrations of SCF were added with or without several concentrations of compound. After culture for 72 hr, the ratios of surviving cells were measured by WST-1.
Concentrations 0~10 μM
Incubation time 72 hr
Animal Experiment
Animal models Female BALB/c nude mice H146 cells tumor xenograft model
Formulation 0.5% methylcellulose
Dosages 30, 100mg/kg twice a day from day 1 to day 21
Administration orally
Chemical Information
Molecular Weight 426.85
Formula C21H19ClN4O4
CAS Number 417716-92-8
Solubility (25°C) DMSO 12 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Boss et al. Br J Cancer. A phase I study of E7080, a multitargeted tyrosine kinase inhibitor, in patients with advanced solid tumours.

[2] Dubbelman et al. J Chromatogr B Analyt Technol Biomed Life Sci. Development and validation of LC-MS/MS assays for the quantification of E7080 and metabolites in various human biological matrices.

[3] Inoue et al. Drug Metab Dispos. Unique metabolic pathway of [(14)C]lenvatinib after oral administration to male cynomolgus monkey.

[4] Glen et al. BMC Cancer. E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion.

[5] Ogino et al. Mol Cancer Ther. E7080 suppresses hematogenous multiple organ metastases of lung cancer cells with nonmutated epidermal growth factor receptor.

[6] Matsui J, et al. Int J Cancer. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition.

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Keywords: Lenvatinib, E7080 supplier, VEGFR/PDGFR, inhibitors, activators

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