1. Protein Tyrosine Kinase/RTK
  2. VEGFR FGFR PDGFR RET c-Kit
  3. Lenvatinib mesylate

Lenvatinib mesylate  (Synonyms: E7080 mesylate)

Cat. No.: HY-10981A Purity: 99.86%
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Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

For research use only. We do not sell to patients.

Lenvatinib mesylate Chemical Structure

Lenvatinib mesylate Chemical Structure

CAS No. : 857890-39-2

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Customer Review

Based on 46 publication(s) in Google Scholar

Other Forms of Lenvatinib mesylate:

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Lenvatinib mesylate

IHC
Proliferation Assay
RT-PCR
WB

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2022 Mar 7;20(1):116.  [Abstract]

    H&E examination of vehicle and Lenvatinib (10 mg/kg daily by oral gavage)-treated tumors revealed markedly increase tumor necrosis and desmoplasia in the Lenvatinib-treated samples.

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: J Oncol. 2022 Oct 18;2022:4537343.

    HepG2 and HepG2/R cells are treated with or without Lenvatinib (20 μM) for 24 h, and indicated proteins are measured by western blots.

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: J Oncol. 2022 Oct 18;2022:4537343.

    HepG2 and HepG2/R cells are treated with indicated doses of Lenvatinib for 24 h, and cellular viabilities are measured.

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Nov 18;7(1):359.  [Abstract]

    Lenvatinib (1000 nM) has demonstrated the ability to significantly inhibit cell proliferation, and knockout of NF1 and DUSP9 significantly blocks the ability of lenvatinib to inhibit cell proliferation as well as the effect on cell number. ​

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Jan;25(1):549-560.  [Abstract]

    The mRNA expression of VEGFR2 in HepG2-WT/Lenvatinib (LR; 5 μM) and Huh7-WT/LR cells. VEGFR2 mRNA expression is up-regulated in HepG2-LR and Huh7LR cells.

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Jan;25(1):549-560.  [Abstract]

    The cell viability is measured by CCK-8 assay at different time intervals (24, 48, 72 and 96 h) when cells are cultured with 5 μM Lenvatinib.

    Lenvatinib mesylate purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Jan;25(1):549-560.  [Abstract]

    The protein expression of VEGFR2 in HepG2-WT/Lenvatinib (LR; 5 μM) and Huh7-WT/LR cells. Western blotting results show the downstream target RAS/MEK/ERK axis of VEGFR2 are obviously up‐regulated in HepG2-LR and Huh7-LR cells compared with their parental cells.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].

    IC50 & Target[1][2][3]

    VEGFR1

    22 nM (IC50)

    VEGFR2

    4 nM (IC50)

    VEGFR3

    5.2 nM (IC50)

    FGFR1

    46 nM (IC50)

    FGFR2

     

    FGFR3

     

    FGFR4

     

    PDGFRα

    51 nM (IC50)

    PDGFRβ

    39 nM (IC50)

    c-Kit

    100 nM (IC50)

    RET

     

    In Vitro

    Lenvatinib mesylate (E7080 mesylate) 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, 100 nM, respectively[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Lenvatinib mesylate (E7080 mesylate) (100 mg/kg, p.o.) is administeredand bevacizumab significantly inhibits local tumor growth at the m.f.p., and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung[3].
    Lenvatinib mesylate (E7080 mesylate) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and imatinib treatment[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    522.96

    Formula

    C22H23ClN4O7S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC4CC4)=O)C(Cl)=C3)C2=C1)N.OS(=O)(C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 31.25 mg/mL (59.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 8.33 mg/mL (15.93 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.86%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9122 mL 9.5610 mL 19.1219 mL 47.8048 mL
    5 mM 0.3824 mL 1.9122 mL 3.8244 mL 9.5610 mL
    10 mM 0.1912 mL 0.9561 mL 1.9122 mL 4.7805 mL
    15 mM 0.1275 mL 0.6374 mL 1.2748 mL 3.1870 mL
    20 mM 0.0956 mL 0.4780 mL 0.9561 mL 2.3902 mL
    25 mM 0.0765 mL 0.3824 mL 0.7649 mL 1.9122 mL
    30 mM 0.0637 mL 0.3187 mL 0.6374 mL 1.5935 mL
    40 mM 0.0478 mL 0.2390 mL 0.4780 mL 1.1951 mL
    50 mM 0.0382 mL 0.1912 mL 0.3824 mL 0.9561 mL
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    Lenvatinib mesylate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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