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

Belinostat (Synonyms: PXD101; PX105684)

Cat. No.: HY-10225 Purity: 99.97%
Handling Instructions

Belinostat 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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 86 In-stock
10 mg USD 78 In-stock
50 mg USD 180 In-stock
100 mg USD 264 In-stock
200 mg USD 420 In-stock
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Customer Review

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

    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

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

    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 MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    H3K9Me2, PTEN, p-AKT, and AKT expression levels are measured in PC9/ER xenograft tumor tissues. β-actin is used as a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Belinostat is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

    IC50 & Target

    IC50: 27 nM (HDAC, in HeLa cells)[1], 82 nM (HDAC6)[2]

    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].

    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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.3141 mL 1.5706 mL 3.1412 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    Belinostat (PXD101) is solubilized in DMSO and stored, and then diluted with appropriate media before use[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]

    Belinostat (PXD101) is dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10% (Mice)[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
    Molecular Weight

    318.35

    Formula

    C₁₅H₁₄N₂O₄S

    CAS No.

    866323-14-0

    SMILES

    O=S(NC1=CC=CC=C1)(C2=CC(/C=C/C(NO)=O)=CC=C2)=O.[(E)]

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Belinostat is dissolved in DMSO to a concentration of 100 mg/mL before diluting to 5 mg/mL using solvent containing (2% Tween-80 and 1% DMSO in saline)[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.97%

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    Product Name:
    Belinostat
    Cat. No.:
    HY-10225
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