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

Lenvatinib  (Synonyms: E7080)

Cat. No.: HY-10981 Purity: 99.84%
COA Handling Instructions

Lenvatinib (E7080) is 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 Chemical Structure

Lenvatinib Chemical Structure

CAS No. : 417716-92-8

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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
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5 mg USD 50 In-stock
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10 mg USD 70 In-stock
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50 mg USD 150 In-stock
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100 mg USD 228 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Lenvatinib:

Top Publications Citing Use of Products

    Lenvatinib purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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 purchased from MCE. 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.

    Lenvatinib purchased from MCE. 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 purchased from MCE. 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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Lenvatinib (E7080) is 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 (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[3].

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

    In Vivo

    Lenvatinib (E7080) (100 mg/kg, p.o.) 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 (E7080) 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 STI571 treatment[4].

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

    Clinical Trial
    Molecular Weight

    426.85

    Formula

    C21H19ClN4O4

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 12.78 mg/mL (29.94 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3427 mL 11.7137 mL 23.4274 mL
    5 mM 0.4685 mL 2.3427 mL 4.6855 mL
    10 mM 0.2343 mL 1.1714 mL 2.3427 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% Methylcellulose/saline water

      Solubility: 6.67 mg/mL (15.63 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.64 mg/mL (1.50 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.84%

    References
    Cell Assay
    [1]

    H146 (1.2×103 cells/50 μL/well) in SFM containing 0.5% BSA are cultured in 96-well multi-plates. After overnight culture at 37°C, SFM (150 μL/well) containing 0.5% FBS and several concentrations of SCF are added with or without several concentrations of compound. After culture for 72 hr, the ratios of surviving cells are measured by WST-1.

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

    Animal Administration
    [1]

    Female BALB/c nude mice (8-12 weeks old, 20-25 g) are maintained under clean-room conditions. H146 tumor cells (6.5×106) are implanted subcutaneously (s.c.) into the flank region of mice. Twelve days after inoculation, mice are randomized into control (n=12) and treatment (n=6 or n=5) groups and this point in time is identified as day 1. Lenvatinib and STI571, and VEGF neutralization antibody are suspended in 0.5% methylcellulose and saline, respectively, and administered orally twice a day for lenvatinib and STI571 and twice a week for antibody from day 1 to day 21. Tumor volume is measured on the indicated days and calculated. Antitumor activity is shown as a relative tumor volume (RTV=calculated tumor volume at indicated days/volume on day 1).

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

    References
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    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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    Product Name:
    Lenvatinib
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