2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Gamabufotalin

Gamabufotalin  (Synonyms: Gamabufagin)

Cat. No.: HY-N0883 Purity: 99.96%
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Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.

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

Gamabufotalin Chemical Structure

Gamabufotalin Chemical Structure

CAS No. : 465-11-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 336 In-stock
Solution
10 mM * 1 mL in DMSO USD 336 In-stock
Solid
1 mg USD 145 In-stock
5 mg USD 306 In-stock
10 mg USD 540 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 8 publication(s) in Google Scholar

Gamabufotalin Related Antibodies

Top Publications Citing Use of Products

    Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 12.  [Abstract]

    Gamabufotalin (CS-6; 15, 20, 25 nM; 48 h) significantly increases the expression of cleaved PARP/PARP, caspase-3/caspase-3, and Bax and decreases the expression of Bcl-2 in Hep3B cells.

    Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 12.  [Abstract]

    Gamabufotalin (CS-6; 10-1000 nM; 48 h) reduces the viability of Hep3B and Huh7 cells in a dose-dependent manner.

    Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 12.  [Abstract]

    Gamabufotalin (CS-6; 15, 20, 25 nM; 48 h) inhibits the proliferation of Hep3B and Huh7 cells in a dose-dependent manner.

    Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 12.  [Abstract]

    Gamabufotalin (CS-6; 25 nM; 15 min) significantly increases the formation of yellow-spotted autophagosomes (GFP+RFP+) and red-spotted autolysosomes (GFP-RFP+) in Hep3B and Huh7 cells.

    View All VEGFR Isoform Specific Products:

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.

    In Vitro

    Gamabufotalin (0-500 nM, 48 h) inhibits cell viability of human lung cancer A549, H1299, H322 cells, and inhibits colony formation and migration (0-100 nM, 48 h), with no cytotoxicity in human normal lung cell line (HLF cells)[1].
    Gamabufotalin (0-100 nM, 12-48 h) inhibits COX-2 expression and inhibits NF-κB and p300 translocation in A549 cells[1].
    Gamabufotalin (0-100 nM, 12-48 h) induces apoptosis by activating the cytochrome c release and caspase-dependent apoptotic pathway in A549 cells[1].
    Gamabufotalin (0-100 nM, 48 h) induces hyperphosphorylation of p38, increases the expression of ATP1A3 and decreases AQP4 expression in U87 cells[3].
    Gamabufotalin (0-50 nM, 24 h) inhibits VEGF (50 ng/mL)-induced angiogenesis in an HUVECs in vitro angiogenesis tube formation assay[4].

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

    Gamabufotalin Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: A549 cells
    Concentration: 0-100 nM
    Incubation Time: 12-48 h
    Result: Increase the expression levels of the cleaved caspase-3, caspase-9 and PARP.
    Induced the release of cyt c from mitochondria to cytosol.

    Immunofluorescence[1]

    Cell Line: A549 cells
    Concentration: 0-100 nM
    Incubation Time: 12-48 h
    Result: Inhibited translocation of the NF-κB p65/p50 proteins from cell cytoplasm to nucleus, and induced p300 into the cytoplasm.
    In Vivo

    Gamabufotalin (5 and 20 mg/kg/day, i.p., for 17 days) inhibits tumor growth in the A549-xenografts mice[1].
    Gamabufotalin (1 mg/kg, i.p., three times per week) together with Temozolomide (HY-17364) (20 mg/kg. i.p., three times per week) shows a synergistic antitumor effect, and inhibits tumor growth and prolongs mice survival in mice U87 xenografts[3].

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

    Animal Model: A549-xenografts mice[1]
    Dosage: 5 and 20 mg/kg/day
    Administration: i.p., for 17 days
    Result: Reduced tumor volume and the tumor weights.
    Decreased COX-2 and p-p65 level in tumors.
    Molecular Weight

    402.52

    Formula

    C24H34O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@]([C@@H](C(C=C1)=COC1=O)CC2)(C[C@@H](O)[C@@]3([H])[C@@]4([H])CC[C@@]5([H])[C@@]3(CC[C@H](O)C5)C)[C@]24O
    Structure Classification
    Initial Source

    toad
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (124.22 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 2.4843 mL 12.4217 mL 24.8435 mL
    5 mM 0.4969 mL 2.4843 mL 4.9687 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
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    C2

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    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: ≥ 2.5 mg/mL (6.21 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.21 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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.
    Purity & Documentation

    Purity: 99.96%

    COA (254 KB) LCMS (114 KB)

    Handling Instructions (2659 KB)
    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, 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 2.4843 mL 12.4217 mL 24.8435 mL 62.1087 mL
    5 mM 0.4969 mL 2.4843 mL 4.9687 mL 12.4217 mL
    10 mM 0.2484 mL 1.2422 mL 2.4843 mL 6.2109 mL
    15 mM 0.1656 mL 0.8281 mL 1.6562 mL 4.1406 mL
    20 mM 0.1242 mL 0.6211 mL 1.2422 mL 3.1054 mL
    25 mM 0.0994 mL 0.4969 mL 0.9937 mL 2.4843 mL
    30 mM 0.0828 mL 0.4141 mL 0.8281 mL 2.0703 mL
    40 mM 0.0621 mL 0.3105 mL 0.6211 mL 1.5527 mL
    50 mM 0.0497 mL 0.2484 mL 0.4969 mL 1.2422 mL
    60 mM 0.0414 mL 0.2070 mL 0.4141 mL 1.0351 mL
    80 mM 0.0311 mL 0.1553 mL 0.3105 mL 0.7764 mL
    100 mM 0.0248 mL 0.1242 mL 0.2484 mL 0.6211 mL
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    Gamabufotalin 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.

    Keywords:

    Gamabufotalin465-11-2GamabufaginVEGFRVascular endothelial growth factor receptorA549H1299H322NSCLCcancerInhibitorinhibitorinhibit

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