| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Lenvatinib mesylate (also known as E-7080, E7080, ER-203492-00; Lenvima), the mesylate salt of lenvatinib, is a multi-targeted and orally bioavailable inhibitor of VEGFR2(KDR)/VEGFR3(Flt-4) approved in 2015 for the treatment of differentiated thyroid cancer. In cell-free assays, it is less potent against VEGFR1/Flt-1 and ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β. Its IC50 values for VEGFR2/VEGFR3 are 4 nM and 5.2 nM, respectively.
| Targets |
RET; FGFR4; FGFR2; FGFR3; VEGFR1 (IC50 = 22 nM); VEGFR2 (IC50 = 4 nM); VEGFR3 (IC50 = 5.2 nM); FGFR1 (IC50 = 46 nM); PDGFRα (IC50 = 51 nM); PDGFRβ (IC50 = 39 nM); c-Kit (IC50 = 100 nM)
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| ln Vitro |
Lenvatinib mesylate (E7080 mesylate) has IC50 values of 4, 5.2, and 22 nM for VEGFR1/Flt-1, VEGFR2(KDR), and VEGFR3(Flt-4), respectively. With IC50 values of 51, 39, 46, and 100 nM, respectively, lenitinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT[3].
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| ln Vivo |
Lenvatinib mesylate (E7080 mesylate) (100 mg/kg, p.o.) also significantly inhibits metastasis to both distant lung and regional lymph nodes after treatment is completed, and bevacizumab significantly inhibits local tumor growth at the m.f.p.[3].
Lenvatinib mesylate (E7080 mesylate) has a dose-dependent effect on the H146 tumor, causing tumor regression at 100 mg/kg in the H146 xenograft model and inhibiting the growth of the tumor at 30 and 100 mg/kg (BID, QDx21). Anti-CD31 antibody IHC analysis reveals that lenvatinib at 100 mg/kg reduces microvessel density more than imatinib treatment and anti-VEGF antibody[4]. |
| Enzyme Assay |
Tyrosine kinase assays using recombinant receptor kinase domains are carried out by HTRF (KDR, VEGFR1, FGFR1, c-Met, EGFR) and ELISA (PDGFRβ). In each experiment, four microliters of successive dilutions of E7080 are combined with ten microliters of enzyme, sixteen microliters of poly (GT) solution (250 ng), and ten microliters of ATP solution (1 μM ATP) in a 96-well round plate (final DMSO concentration is 0.1%). No enzyme is introduced to blank wells. Test articles are not added to control wells. Addition of ATP solution to each well starts the kinase reaction. Each well's reaction mixture is mixed with 10 μL of 0.5 M EDTA to halt the reaction after a 30-minute incubation period at 30°C. The reaction mixture is supplemented with dilution buffer appropriate for each kinase assay. The HTRF assay involves transferring 50 μL of the reaction mixture to a 96-well 1/2 area black EIA/RIA plate, adding 50 μL of HTRF solution per well, and measuring the fluorescence of the reaction mixture using a time-resolved fluorescence detector at 620 and 665 nm for emission and 337 nm for excitation. This allows for the determination of kinase activity. For the ELISA, 96-well polystyrene plates coated with avidin are incubated at room temperature for 30 minutes with 50 μL of the reaction mixture. PY20-HRP solution (70 μL/well) is added to the reaction mixture after washing with wash buffer, and it is then incubated at room temperature for 30 minutes. TMB reagent (100 μL/well) is added to each well following washing with wash buffer. One milligram of H3PO4 (100 μL/well) is added to each well after a few minutes (10–30 minutes). The measurement of absorbance at 450 nm using a microplate reader yields the kinase activity.
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| Cell Assay |
In a 96-well plate, 1,000 HUVECs (1,000 cells in each well in serum-free medium containing 2% fetal bovine serum) and 5,000 L6 rat skeletal muscle myoblasts (5,000 cells in each well in serum-free DMEM) are added, and the plate is left to incubate overnight. To each well, E7080, VEGF (20 ng/mL) or FGF-2 (20 ng/mL) containing 2% fetal bovine serum, and PDGFβ (40 ng/mL) are added. Following three days of incubation, the WST-1 reagent is used to calculate the ratios of surviving cells. Samples are replicated and three independent experiments are conducted for the proliferation assay.
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| Animal Protocol |
Female BALB/c nude mice
30 & 100 mg/kg p.o. |
| References |
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| Molecular Formula |
C22H23CLN4O7S
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|---|---|
| Molecular Weight |
522.96
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| Exact Mass |
522.0975980
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| Elemental Analysis |
C, 50.53; H, 4.43; Cl, 6.78; N, 10.71; O, 21.42; S, 6.13
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| CAS # |
857890-39-2
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| Related CAS # |
Lenvatinib;417716-92-8
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| Appearance |
White to off-white solid powder
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| SMILES |
COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl.CS(=O)(=O)O
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| InChi Key |
HWLFIUUAYLEFCT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19ClN4O4.CH4O3S/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11;1-5(2,3)4/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28);1H3,(H,2,3,4)
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| Chemical Name |
4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide;methanesulfonic acid
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| Synonyms |
E-7080 mesylate; E7080; E 7080; ER-203492-00 mesylate; Lenvatinib mesylate; Brand name Lenvima
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose: 30 mg/kg |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9122 mL | 9.5610 mL | 19.1219 mL | |
| 5 mM | 0.3824 mL | 1.9122 mL | 3.8244 mL | |
| 10 mM | 0.1912 mL | 0.9561 mL | 1.9122 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03477175 | Active Recruiting |
Drug: E7080 Drug: Comparator Drug |
Solid Tumors | Eisai Inc. | August 16, 2018 | Phase 2 |
| NCT05339581 | Not yet recruiting | Drug: Sintilimab Drug: Tislelizumab |
Liver Cancer Portal Vein Thrombosis |
RenJi Hospital | May 20, 2022 | Not Applicable |
| NCT05617859 | Recruiting | Drug: Lenvatinib mesylate capsule |
Effectiveness Sexuality |
Henan Cancer Hospital | April 30, 2023 | Phase 2 |
| NCT05296512 | Recruiting | Drug: Lenvatinib Drug: Pembrolizumab |
Ovarian Clear Cell Carcinoma Gynecologic Cancer |
Elizabeth K. Lee MD | September 23, 2022 | Phase 2 |
| NCT05342194 | Not yet recruiting | Drug: Toripalimab Drug: Placebo IV |
Intrahepatic Cholangiocarcinoma | Shanghai Junshi Bioscience Co., Ltd. |
October 1, 2022 | Phase 3 |
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