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.
Cited by 7 Publications
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Real-time monitoring of cytotoxic effect on HT29 cells using RTCA. (A) E7080
Chin J Cancer Res 2013 25(5), 572-84. Lenvatinib (E7080) purchased from Selleck.
Inhibitors of tyrosine kinase receptor suppressed the in vitro angiogenesis of HUVECs. The angiogenesis of HUVECs was evaluated in the absence (control in A) or presence of CP-673451 (5 nM), a selective inhibitor of PDGFR or E7080 (50 nM), an active inhibitor for multiple tyrosine kinase receptors for 6 h. The two agents only inhibit the kinase activity of the relative tyrosine kinase receptors, but do not cause a toxic effect to the cells in the concentration used in this study (Roberts et al., 2005 ; Wiegering et al., 2014). For quantification, the values for the pattern recognition, branch point and total capillary tube length are described in the Methods section. Representative microscopic fields are shown in Panel A. The suppressive effects of the inhibitors on angiogenesis of HUVECs are shown in B, C and D. The data are expressed relative to that of the control cells without exposure to the inhibitor. N = 5, *P < 0.05 and **P < 0.01 versus the control cells.
Environ Toxicol Pharmacol, 2016, 46:168-73. Lenvatinib (E7080) purchased from Selleck.
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Choose Selective VEGFR Inhibitors
|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 warmed (93.7 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02702388||Recruiting||Thyroid Cancer||Eisai Inc.||June 8 2017||Phase 2|
|NCT02973997||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 AJCC v7|Stage III Thyroid Gland Follicular Carcinoma AJCC v7|Stage III Thyroid Gland Papillary Carcinoma AJCC v7|Stage IV Thyroid Gland Follicular Carcinoma AJCC v7|Stage IV Thyroid Gland Papillary Carcinoma AJCC v7|Stage IVA Differentiated Thyroid Gland Carcinoma AJCC v7|Stage IVA Thyroid Gland Follicular Carcinoma AJCC v7|Stage IVA Thyroid Gland Papillary Carcinoma AJCC v7|Stage IVB Differentiated Thyroid Gland Carcinoma AJCC v7|Stage IVB Thyroid Gland Follicular Carcinoma AJCC v7|Stage IVB Thyroid Gland Papillary Carcinoma AJCC v7|Stage IVC Differentiated Thyroid Gland Carcinoma AJCC v7|Stage IVC Thyroid Gland Follicular Carcinoma AJCC v7|Stage IVC Thyroid Gland Papillary Carcinoma AJCC v7|Tall Cell Variant Thyroid Gland Papillary Carcinoma|Thyroid Gland Oncocytic Follicular Carcinoma||Academic and Community Cancer Research United|National Cancer Institute (NCI)||February 7 2018||Phase 2|
|NCT02657369||Active not recruiting||Thyroid Cancer Anaplastic||Eisai Inc.||July 7 2016||Phase 2|
|NCT02726503||Recruiting||Anaplastic Thyroid Cancer||Translational Research Center for Medical Innovation Kobe Hyogo Japan||April 4 2016||Phase 2|
|NCT03008369||Recruiting||Malignant Adrenal Gland Pheochromocytoma|Malignant Paraganglioma|Metastatic Adrenal Gland Pheochromocytoma||Mayo Clinic|National Cancer Institute (NCI)||May 31 2017||Phase 2|
|NCT00946153||Completed||Hepatocellular Carcinoma||Eisai Co. Ltd.|Eisai Inc.||July 31 2009||Phase 1|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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