Belinostat (PXD101)

Catalog No.S1085

Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.

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Belinostat (PXD101) Chemical Structure

Belinostat (PXD101) Chemical Structure
Molecular Weight: 318.35

Validation & Quality Control

Customer Product Validation(5)

Quality Control & MSDS

Related Compound Libraries

Belinostat (PXD101) is available in the following compound libraries:

HDAC Inhibitors with Unique Features

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Product Description

Biological Activity

Description Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.
Targets HDAC [1]
(Cell-free assay)
IC50 27 nM
In vitro Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. Belinostat could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. [1] Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. [2] The growth inhibitory activity of belinostat on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. Belinostat could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. [3] A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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... Click to View More Cell Line Experimental Data

In vivo Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. [1] Belinostat also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. [2] Belinostat monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of Belinostat (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. [3] Combining with bortezomib, Belinostat results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft. [5]
Features Lead compound of Topotarget.

Protocol(Only for Reference)

Kinase Assay: [1]

Histone Deacetylase Activity Subconfluent cultures are harvested and washed twice in ice cold PBS and pelleted by centrifugation at 200 × g for 5 min. The cell pellet is resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl] and lysed by three freeze (dry ice) thaw (30 °C water bath) cycles. Cell debris is removed by centrifugation at 1.2 × 104 g for 5 min, and the supernatant is stored at −80 °C. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK corresponding to the 20 NH2-terminal residues) is acetylated by a recombinant protein containing the hypoxanthine-aminopterin-thymidine domain of p300, using [3H]acetyl CoA as a source of acetate. H4 peptide (100 μg) is mixed with hypoxanthine-aminopterin-thymidine buffer (50 mM Tris HCl pH 8.0, 5% glycerol, 50 mM KCl, and 0.1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzenesulfonylfluoride, 1 × complete protease inhibitors, 50 μL of purified p300, and 1.85 m [3H]acetyl CoA (4.50Ci/mmol) in a final volume of 300 μL and incubated at 30 °C for 45 min. The p300 protein is removed by incubation with 20 μL of 50% Ni-agaroase beads for 1 hour at 4 °C and centrifugation. The supernatant is applied to a 2 mL Sephadex G15 column, and the flow through is collected. One milliliter of distilled H2O is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled H2O has been added, and ∼40 fractions are collected. Three microliters of each fraction are diluted in 2 mL of scintillation fluid and counted in a scintillation counter to identify the fractions containing the labeled peptide. These fractions are pooled, and 1 μL of the combined sample is measured to assess the radioactivity in every peptide batch (3-7×103 cpm/μL). 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 1.2× 104 g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted.

Cell Assay: [1]

Cell lines A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852
Concentrations 0.016 - 10 μM
Incubation Time 24 hours
Method Tumor cell lines are seeded in 5 mL of medium at a density of 8 × 104 cells/25 cm2 flask and incubated for 48 hours. Cells are exposed to Belinostat (0.016 to 10 μM) for 24 hours. 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 0.5-2× 103 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 defined as the concentration of belinostat required to reduce the number of colonies to 50% of that of the control untreated cells.

Animal Study: [1]

Animal Models A2780, A2780/cp70 and HCT116 cells are injected s.c. into the right flank of CD1 nu/nu mice.
Formulation Dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10%
Dosages ≤40 mg/kg
Administration Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Plumb JA, et al. Mol Cancer Ther, 2003, 2(8), 721-728.

[2] Buckley MT, et al. J Transl Med, 2007, 5:49.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02701673 Withdrawn Lymphoma M.D. Anderson Cancer Center June 2016 Phase 1|Phase 2
NCT02737046 Not yet recruiting Adult T-cell Leukemia-Lymphoma|ATLL University of Miami April 2016 Phase 2
NCT02680795 Recruiting Solid Tumors|Hematological Malignancies Spectrum Pharmaceuticals, Inc March 2016 Phase 1
NCT02679131 Recruiting Relapsed/Refractory Solid Tumors/Hematological Malignancies Spectrum Pharmaceuticals, Inc March 2016 Phase 1
NCT02532192 Withdrawn Lymphoma M.D. Anderson Cancer Center|Spectrum Pharmaceuticals, Inc December 2015 Phase 1

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Chemical Information

Download Belinostat (PXD101) SDF
Molecular Weight (MW) 318.35
Formula

C15H14N2O4S

CAS No. 414864-00-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC726630, PX-105684
Solubility (25°C) * In vitro DMSO 64 mg/mL (201.03 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 12 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Propenamide, N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-

Customer Product Validation (5)


Click to enlarge
Rating
Source Breast Cancer Res Treat 2012 131, 777-789. Belinostat (PXD101) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 cells, MDA-MB-468 cells
Concentrations 0.5-10 μM
Incubation Time 24 h
Results In both MDA-MB-231 and MDA-MB-468 cell lines, exposure to these compounds produced significant global increase of nuclear H3K4me2,which is the specific substrate of LSD1.The enhanced level of histone methylation by PXD101 and other HDAC inhibitors parallels the increase of acetylation of histone 3.

Click to enlarge
Rating
Source Breast Cancer Res Treat 2010 131(3), 777-789. Belinostat (PXD101) purchased from Selleck
Method MTT growth inhibition and drug combination index (CI) analysis
Cell Lines MDA-MB-231 cells
Concentrations
Incubation Time 48 h
Results At very low dose combination (fractional growth inhibition,Fa=0.9), synergistic growth inhibition (CI<1) was observed between pargyline and HDAC inhibitors PXD101, TSA, MS-275, and LBH-589.At median or higher dose combination (Fa = 0.5 or 0.75), pargyline exhibited synergy with all the HDAC inhibitors tested (CI<1)

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Rating
Source PLoS One 2011 6, e17138. Belinostat (PXD101) purchased from Selleck
Method Western blot, Enzymatic Assays of Class I HDACs Following Immunoprecipitation (IP), Assessment of Baseline and Drug Induced Apoptosis
Cell Lines THP-1 cells
Concentrations 0.7 μM
Incubation Time 3/24 h
Results Treatments with LBH-589, PXD101, and SAHA, but not with the other HDACIs, resulted in hyperacetylation ofa-tubulin, the substrate of HDAC6 (Figure A). IP followed by enzymatic assays revealed that both LBH-589 and PXD101 treatments resulted in the greatest inhibition of HDAC1 activities (>80% relative to control), compared to other HDACIs tested (Figure C). This was accompanied by significantly higher extents of proliferation inhibition (as reflected in percent decrease of live cells relative to untreated cells) and apoptosis (Figures E&F). Essentially the same results were obtained in THP-1 cells when the HDACI treatments were extended to 24 h, though the levels of apoptosis induced by the drugs were substantially higher (Figures B, D, E&F).

Click to enlarge
Rating
Source PLoS One 2011 6, e17138. Belinostat (PXD101) purchased from Selleck
Method Western blot
Cell Lines THP-1 cells
Concentrations 0.7 μM
Incubation Time 3/24 h
Results Effects of PXD101 and other HDACIs on p21, c-Myc, and Bim expression, and in inducing DNA damage (as reflected in cH2AX) were both drug-dependent and time-dependent, as reflected in results at 3h and 24h.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. Belinostat (PXD101) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 Breast cancer cells
Concentrations 0-20 μM
Incubation Time
Results Increased Histone H3 acetylation with PXD101 treatment was observed in MDA-MB-231 Breast cancer cells.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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