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

Lenvatinib  (Synonyms: E7080)

製品番号: HY-10981 純度: 99.84%
COA 取扱説明書

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

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Lenvatinib 構造式

Lenvatinib 構造式

CAS 番号 : 417716-92-8

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg USD 50 在庫あり
10 mg USD 70 在庫あり
50 mg USD 150 在庫あり
100 mg USD 228 在庫あり
200 mg   お問い合わせ  
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カスタマーレビュー

Based on 46 publication(s) in Google Scholar

Other Forms of Lenvatinib:

Lenvatinib 関連抗体

Top Publications Citing Use of Products

顧客検証

IHC
Proliferation Assay
RT-PCR
WB

    Lenvatinib 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 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 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 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 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 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 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.

    VEGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    FGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    PDGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PDGFR PDGFRβ PDGFRα

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    製品説明

    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

     

    体外実験

    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].

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

    Lenvatinib 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    426.85

    分子式

    C21H19ClN4O4
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 12.78 mg/mL (29.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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

    体内:

    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:  5% DMSO    95% (20% SBE-β-CD in Saline)

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

    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:  0.5% Methylcellulose/saline water

      Solubility: 6.67 mg/mL (15.63 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).
    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.
    純度とドキュメンテーション

    純度: 99.84%

    COA (248 KB) HNMR (288 KB) LCMS (265 KB) Elemental Analysis Report (106 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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).

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3427 mL 11.7137 mL 23.4274 mL 58.5686 mL
    5 mM 0.4685 mL 2.3427 mL 4.6855 mL 11.7137 mL
    10 mM 0.2343 mL 1.1714 mL 2.3427 mL 5.8569 mL
    15 mM 0.1562 mL 0.7809 mL 1.5618 mL 3.9046 mL
    20 mM 0.1171 mL 0.5857 mL 1.1714 mL 2.9284 mL
    25 mM 0.0937 mL 0.4685 mL 0.9371 mL 2.3427 mL
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    Lenvatinib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    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.

    Keywords:

    Lenvatinib417716-92-8E7080E 7080E-7080VEGFRFGFRPDGFRc-KitRETVascular endothelial growth factor receptorFibroblast growth factor receptorPlatelet-derived growth factor receptorSCFRCD117Inhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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