1. Apoptosis Autophagy PI3K/Akt/mTOR Cell Cycle/DNA Damage Epigenetics
  2. Apoptosis Autophagy PI3K Akt mTOR PARP Caspase Atg8/LC3
  3. Arenobufagin

Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway.

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CAS 番号 : 464-74-4

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
1 mg $60 在庫あり
5 mg $150 在庫あり
10 mg $240 在庫あり
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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Arenobufagin:

Top Publications Citing Use of Products

    Arenobufagin purchased from MedChemExpress. Usage Cited in: Molecules. 2017 Sep 11;22(9). pii: E1525.  [Abstract]

    A549 and NCI-H460 cells are treated with Arenobufagin at the indicated concentrations for 24 h, and protein extracts are subjected to Western blot assay with indicated antibodies;
    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    0.0001 μM
    Compound: Arenobufagin
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 30181060]
    HepG2 IC50
    0.02 μM
    Compound: Arenobufagin
    Antiproliferative activity against human HepG2 cells by MTT assay
    Antiproliferative activity against human HepG2 cells by MTT assay
    [PMID: 30181060]
    HepG2/Adm IC50
    0.056 μM
    Compound: Arenobufagin
    Antiproliferative activity against human HepG2/ADM cells by MTT assay
    Antiproliferative activity against human HepG2/ADM cells by MTT assay
    [PMID: 30181060]
    MCF7 IC50
    8.88 nM
    Compound: Arenobufagin
    Antiproliferative activity against FAP-alpha deficient human MCF7 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against FAP-alpha deficient human MCF7 cells incubated for 48 hrs by MTT assay
    [PMID: 28595013]
    MDA-MB-231 IC50
    15.67 nM
    Compound: Arenobufagin
    Antiproliferative activity against FAP-alpha deficient human MDA-MB-231 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against FAP-alpha deficient human MDA-MB-231 cells incubated for 48 hrs by MTT assay
    [PMID: 28595013]
    MDA-MB-435 IC50
    22.45 nM
    Compound: Arenobufagin
    Antiproliferative activity against wild type human MDA-MB-435 cells expressing FAP-alpha incubated for 48 hrs by MTT assay
    Antiproliferative activity against wild type human MDA-MB-435 cells expressing FAP-alpha incubated for 48 hrs by MTT assay
    [PMID: 28595013]
    体外実験

    Arenobufagin (10 nM-10 μM, 48-72 h) potently inhibits the growth of both HepG2 and HepG2/ADM cells in a dose- and time-dependent manner, with the IC50 of 20.24 and 7.46 nM after 72 h[1].
    Arenobufagin (20-500 nM, 24 h) increases the percentage of apoptotic (annexin positive) cells in HCC cells[1].
    Arenobufagin (20-500 nM, 48 h) induces a specific cleavage of poly (ADP-ribose) polymerase (PARP) and a decrease in pro-caspase-9 and -3[1].
    Arenobufagin (20 nM, 0-24 h) induces autophagic cell death and a significant increase in LC3-II in HepG2/ADM cells[1].
    Arenobufagin (0-500 nM, 0-24 h) inhibits the activation of PI3K/Akt pathways in HCC cells[1].
    Arenobufagin (0-125 nM, 12-48 h) inhibits cell viability in a dose- and time-dependent manner in HUVECs[2].
    Arenobufagin (5-125 nM, 12-48 h) significantly suppresses VEGF-induced HUVECs viability in a dose- and time-dependent manner[2].
    Arenobufagin (0-50 nM, 6 h) inhibits VEGF-induced endothelial cell migration and invasion[2].

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

    Immunofluorescence[1]

    Cell Line: Hepatoma carcinoma cells
    Concentration: 20, 200, 500 nM
    Incubation Time: 24 h
    Result: Depolarized mitochondrial membrane potential dose-dependently.
    体内実験

    Arenobufagin (3-6 mg/kg, i.p., 28 d) inhibits growth of HepG2/ADM cells xenografts in nude mice[1].
    Arenobufagin (0-10 mg/kg, s.c., 21 d) inhibits VEGF-induced blood vessel formation in C57BL/6J mice[2].

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

    Animal Model: Nude mice with HepG2/ADM xenografts[1]
    Dosage: 3 and 6 mg/kg
    Administration: Intraperitoneal injection (i.p.), 28 d
    Result: Significantly reduced the tumor volume.
    Resulted in remarkable decrease in levels of proliferating cell nuclear antigen, PARP, total and phosphorylated mTOR as well as increase of LC3-II.
    Decreased the degree of phposphorylation of mTOR at Ser2448.
    分子量

    416.51

    分子式

    C24H32O6

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@]([C@@H](C(C=C1)=COC1=O)CC2)(C3=O)[C@]2([C@@](CC[C@@]4([H])[C@@]5(CC[C@H](O)C4)C)([H])[C@]5([H])[C@@H]3O)O

    Structure Classification
    Initial Source

    toad

    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 : 100 mg/mL (240.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 10 mg/mL (24.01 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4009 mL 12.0045 mL 24.0090 mL
    5 mM 0.4802 mL 2.4009 mL 4.8018 mL
    10 mM 0.2401 mL 1.2005 mL 2.4009 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 6.25 mg/mL (15.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (15.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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    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: 99.82%

    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, 6 months; -20°C, 1 month. 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
    Ethanol / DMSO 1 mM 2.4009 mL 12.0045 mL 24.0090 mL 60.0226 mL
    5 mM 0.4802 mL 2.4009 mL 4.8018 mL 12.0045 mL
    10 mM 0.2401 mL 1.2005 mL 2.4009 mL 6.0023 mL
    15 mM 0.1601 mL 0.8003 mL 1.6006 mL 4.0015 mL
    20 mM 0.1200 mL 0.6002 mL 1.2005 mL 3.0011 mL
    DMSO 25 mM 0.0960 mL 0.4802 mL 0.9604 mL 2.4009 mL
    30 mM 0.0800 mL 0.4002 mL 0.8003 mL 2.0008 mL
    40 mM 0.0600 mL 0.3001 mL 0.6002 mL 1.5006 mL
    50 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2005 mL
    60 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0004 mL
    80 mM 0.0300 mL 0.1501 mL 0.3001 mL 0.7503 mL
    100 mM 0.0240 mL 0.1200 mL 0.2401 mL 0.6002 mL
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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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    Inquiry Information

    製品名:
    Arenobufagin
    製品番号:
    HY-N0876
    数量:
    MCE 日本正規代理店: