1. Cell Cycle/DNA Damage Epigenetics Autophagy
  2. HDAC Autophagy
  3. Belinostat

Belinostat  (Synonyms: PXD101; PX105684)

Cat. No.: HY-10225 Purity: 99.95%
COA Handling Instructions

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

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

Belinostat Chemical Structure

Belinostat Chemical Structure

CAS No. : 866323-14-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 86 In-stock
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10 mg USD 78 In-stock
50 mg USD 180 In-stock
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Customer Review

Based on 25 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Belinostat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.  [Abstract]

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

    Belinostat purchased from MedChemExpress. Usage Cited in: Invest New Drugs. 2016 Oct;34(5):552-64.  [Abstract]

    The phenotypic characteristics of LN-229 and LN-18 glioblastoma cells after 48 h of Belinostat (Bel) treatment. Representative photographs are shown. Morphological effects induced by 0.5 and 2 μM Bel after 48-h treatment, evaluated by phase contrast microscopy (magnification 100×) (a, c); evaluated by the acridine orange/ethidium bromide staining, shown by fluorescence microscopy (magnification 200×) (b, d). Markedly enlarged cells with bright yellow, condensed nuclei are visible. Evident reduct
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

    IC50 & Target[1][2]

    HDAC6

    82 nM (IC50)

    HDAC

    27 nM (IC50, Hela cell)

    In Vitro

    Belinostat (PXD101) induces a concentration-dependent (0.2-5 μM) increase in acetylation of histone H4 in tumor cell lines. Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. Belinostat inhibits the growth of a number of human tumor cell lines in vitro with IC50s determined by a clonogenic assay in the range 0.2-3.4 μM[1]. Belinostat (PXD101) is a potent histone deacetylase (HDAC) inhibitor, potently inhibits the enzymatic activity of purified recombinant HDAC6 (IC50 of 82 nM)[2].

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

    In Vivo

    Treatment of nude mice bearing human ovarian and colon tumor xenografts with Belinostat (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice. Growth delay is also observed for xenografts of cisplatin-resistant ovarian tumor cells. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with Belinostat (PXD101). The inhibition of growth of human tumor xenografts in mice, with no apparent toxicity[1]. Belinostat (PXD101) displays single-agent antitumor activity on human A2780 ovarian cancer s.c. xenografts which is enhanced via combination therapy with Carboplatin[2].

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

    Clinical Trial
    Molecular Weight

    318.35

    Formula

    C15H14N2O4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(NC1=CC=CC=C1)(C2=CC(/C=C/C(NO)=O)=CC=C2)=O

    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 : 100 mg/mL (314.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 25 mg/mL (78.53 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1412 mL 15.7060 mL 31.4120 mL
    5 mM 0.6282 mL 3.1412 mL 6.2824 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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    Volume
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    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.85 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.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (6.53 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.
    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: 99.95%

    References
    Kinase Assay
    [1]

    For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of Belinostat. The reaction is started by the addition of 2 μL of [3H]labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples are incubated at 37°C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [3H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 12,000× g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted[1].

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

    Cell Assay
    [1]

    The human ovarian cell line A2780 and Cisplatin (A2780/cp70) and Doxorubicin (2780AD) resistant derivatives are grown in RPMI 1640 supplemented with glutamine (2 mM) and FCS (10%). The human colon (HCT116 and HT29), melanoma (HS852), prostate (PC3), lung (CALU-3), and breast (MCF7) cell lines are grown in RPMI 1640 and the rest in DMEM supplemented as above. The human non-small cell lung cancer cell line WIL is grown in DMEM supplemented as above. Drug sensitivity is determined by a clonogenic assay. Briefly, cells are plated in 5 mL of medium at a density of 8×104 cells/25 cm2 flask and allowed to attach and grow for 48 h. Cells are exposed to Belinostat (five concentrations from 0.016 to 10 μM) for 24 h. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 500-2000 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10-15 days at 37°C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 (mean±SE of three experiments) defined as the concentration of drug required to reduce the number of colonies to 50% of that of the control untreated cells[1].

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

    Animal Administration
    [1]

    Mice[1]
    For the human tumor xenograft studies, monolayer cultures are harvested with trypsin/EDTA (0.25%/1 mM in PBS) and resuspended in PBS. About 107 cells are injected s.c. into the right flank of athymic nude mice (CD1 nu/nu mice). After 10-15 days when the mean tumor diameter is ≥0.5 cm, animals are randomized into groups of six for experiments. Belinostat is dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10% and is administered i.p. at the times specified. This formulation gives sufficient solubility for doses of ≤ 40 mg/kg. Mice are weighed daily, and tumor volumes are estimated by caliper measurements assuming spherical geometry (volume=d3×π/6).

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

    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
    Ethanol / DMSO 1 mM 3.1412 mL 15.7060 mL 31.4120 mL 78.5299 mL
    5 mM 0.6282 mL 3.1412 mL 6.2824 mL 15.7060 mL
    10 mM 0.3141 mL 1.5706 mL 3.1412 mL 7.8530 mL
    15 mM 0.2094 mL 1.0471 mL 2.0941 mL 5.2353 mL
    20 mM 0.1571 mL 0.7853 mL 1.5706 mL 3.9265 mL
    25 mM 0.1256 mL 0.6282 mL 1.2565 mL 3.1412 mL
    30 mM 0.1047 mL 0.5235 mL 1.0471 mL 2.6177 mL
    40 mM 0.0785 mL 0.3926 mL 0.7853 mL 1.9632 mL
    50 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5706 mL
    60 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3088 mL
    DMSO 80 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9816 mL
    100 mM 0.0314 mL 0.1571 mL 0.3141 mL 0.7853 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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