Molecular Weight(MW): 426.85
Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Phase 3.
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Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
Asian Pac J Cancer Prev 2014 15(7), 3113-21. Lenvatinib (E7080) purchased from Selleck.
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|Description||Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Phase 3.|
E7080, as a potent inhibitor of in vitro angiogenesis, shows a significantly inhibitory effect on VEGF/KDR and SCF/Kit signaling. According to the in vitro receptor tyrosine and serine/threonine kinase assays, E7080 inhibits Flt-1, KDR, Flt-4 with IC50 of 22, 4.0 and 5.2 nM, respectively. In addition to these kinases, E7080 also inhibits FGFR1 and PDGFR tyrosine kinases with IC50 value of 46, 51 and 100 nM for FGFR1, PDGFRα and PDGFRβ, respectively.  E7080 potently inhibits phosphorylation of VEGFR2 (IC50, 0.83 nM) and VEGFR3 (IC50, 0.36 nM) in HUVECs which is stimulated by VEGF and VEGF-C, respectively.  A recent study shows that E7080 treatment (both at 1 μM and 10 μM) results in a significant inhibition of cell migration and invasion by inhibiting FGFR and PDGFR signaling. 
|In vivo||When orally administrated in a H146 xenograft model, E7080 inhibits the growth of H146 tumor at 30 and 100 mg/kg in a dose-dependent manner and leads to tumor regression at 100 mg/kg. Furthermore, E7080 at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and imatinib treatment.  E7080 significantly inhibits local tumor growth in a MDA-MB-231 mammary fat pad (m.f.p.) model with RTVs (calculated tumor volume on day 8/tumor volume on day 1) of 0.81, and reduces both angiogenesis and lymphangiogenesis of established metastatic nodules of MDA-MB-231 tumor in the lymph nodes. |
In vitro kinase assay :Tyrosine kinase assays are performed by HTRF (KDR, VEGFR1, FGFR1, c-Met, EGFR) and ELISA (PDGFRβ), using the recombinant kinase domains of receptors. In both assays, 4 μL of serial dilutions of E7080 are mixed in a 96-well round plate with 10 μL of enzyme, 16 μL of poly (GT) solution (250 ng) and 10 μL of ATP solution (1 μM ATP) (final concentration of DMSO is 0.1%). In wells for blanks, no enzyme is added. In control wells no test article is added. The kinase reaction is initiated by adding ATP solution to each well. After 30-minute incubation at 30°C, the reaction is stopped by adding 0.5 M EDTA (10 μL/well) to the reaction mixture in each well. Dilution buffer adequate to each kinase assay is added to the reaction mixture. In the HTRF assay, 50 μL of the reaction mixture is transferred to a 96-well 1/2 area black EIA/RIA plate, HTRF solution (50 μL/well) is added to the reaction mixture, and then kinase activity is determined by measurement of fluorescence with a time-resolved fluorescence detector at an excitation wavelength of 337 nm and an emission wavelengths of 620 and 665 nm. In the ELISA, 50 μL of the reaction mixture is incubated in avidin coated 96-well polystyrene plates at room temperature for 30 minutes. After washing with wash buffer, PY20-HRP solution (70 μL/well) is added and the reaction mixture is incubated at room temperature for 30 minutes. After washing with wash buffer, TMB reagent (100 μL/well) is added to each well. After several minutes (10–30 minutes), 1 M H3PO4 (100 μL/well) is added to each well. Kinase activity is determined by measurement of absorbance at 450 nm with a microplate reader.
|In vitro||DMSO||40 mg/mL (93.7 mM) warming|
|In vivo||0.5% methylcellulose||30 mg/mL|
* 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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02657369||Recruiting||Thyroid Cancer, Anaplastic||Eisai Inc.||July 7, 2016||Phase 2|
|NCT02432274||Recruiting||Tumors|Solid Malignant Tumors|Osteosarcoma|Differentiated Thyroid Cancer (DTC)||Eisai Limited|Eisai Inc.||December 29, 2014||Phase 1|Phase 2|
|NCT02788708||Recruiting||Fallopian Tube Carcinoma|Recurrent Ovarian Cancer|Primary Peritoneal Carcinoma|Recurrent Endometrial Cancer||Floor Backes|Eisai Inc.|Ohio State University Comprehensive Cancer Center||May 27, 2016||Phase 1|
|NCT02501096||Recruiting||Tumors||Eisai Inc.||July 22, 2015||Phase 1|Phase 2|
|NCT03009292||Not yet recruiting||Solid Tumor||Eisai Inc.||January 2019||Phase 1|
|NCT02973997||Not yet recruiting||Columnar Cell Variant Thyroid Gland Papillary Carcinoma|Follicular Variant Thyroid Gland Papillary Carcinoma|Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Thyroid Gland Carcinoma|Stage III Differentiated Thyroid Gland Carcinoma|Stage III Thyroid Gland Follicular Carcinoma|Stage III Thyroid Gland Papillary Carcinoma|Stage IV Thyroid Gland Follicular Carcinoma|Stage IV Thyroid Gland Papillary Carcinoma|Stage IVA Differentiated Thyroid Gland Carcinoma|Stage IVA Thyroid Gland Follicular Carcinoma|Stage IVA Thyroid Gland Papillary Carcinoma|Stage IVB Differentiated Thyroid Gland Carcinoma|Stage IVB Thyroid Gland Follicular Carcinoma|Stage IVB Thyroid Gland Papillary Carcinoma|Stage IVC Differentiated Thyroid Gland Carcinoma|Stage IVC Thyroid Gland Follicular Carcinoma|Stage IVC Thyroid Gland Papillary Carcinoma|Tall Cell Variant Thyroid Gland Papillary Carcinoma|Thyroid Gland Oncocytic Follicular Carcinoma||Academic and Community Cancer Research United|National Cancer Institute (NCI)||April 2017||Phase 2|
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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