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Belinostat (PXD101) Catalog No.GC15962

Hydroxamate-type HDAC inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$52.00
In stock
10mg
$44.00
In stock
50mg
$147.00
In stock
100mg
$240.00
In stock
200mg
$443.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Inhibitory activities

For activity assays, the reaction was 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 PXD101. The reaction was started by the addition of 2 μl of [3H]labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples were incubated at 37℃ 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 was extracted into 750 μl of ethyl acetate, and samples were centrifuged at 12,000×g for 5 min. The upper phase (600 μl) was transferred to 3 ml of scintillation fluid and counted.

Cell experiment [2]:

Cell lines

The human urinary bladder carcinoma cell lines 5637, T24, J82 and RT4.

Preparation method

Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1-5 μM; 48 h.

Applications

In human urinary bladder carcinoma cell lines, belinostat (PXD101) inhibits cell proliferation in a dose dependent way with IC50 values of 1.0, 3.5, 6.0 and 10.0 μM in 5637, T24, J82 and RT4 cell lines, respectively. Belinostat (PXD101) (5 μM) decreases in cell growth and proliferation by 71%, 51%, 41% and 23% in 5637, T24, J82 and RT4 cell lines, respectively. Also, belinostat reduces cells in the S phase and increases cells in the G0-G1 phase.

Animal experiment [2]:

Animal models

UPII-Ha-ras transgenic mice.

Dosage form

100 mg/kg; 5 days each week for 3 weeks; intraperitoneal (IP) injections.

Preparation method

Dissolved in L-Arginine to give a final concentration of 20 mg/ml.

Applications

In UPII-Ha-ras transgenic mice, belinostat reduces the weights of Ras-expressing bladders of the male and female transgenic mice by 50% and 36%, respectively. Belinostat inhibits progression of bladder disease. Belinostat shows no detectable toxicity as evaluated by weight.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Plumb JA, Finn PW, Williams RJ, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther, 2003, 2(8): 721-728.

[2]. Buckley MT, Yoon J, Yee H, et al. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. J Transl Med, 2007, 5: 49.

Chemical Properties

Cas No. 414864-00-9 SDF
Synonyms PXD-101, PXD 101, PX105684, PX-105684
Chemical Name (E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
Canonical SMILES C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO
Formula C15H14N2O4S M.Wt 318.35
Solubility ≥ 15.92 mg/mL in DMSO, ≥ 44.1 mg/mL in EtOH with ultrasonic Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

Belinostat (also known as PXD101) is a novel and potent hydroxamate-type inhibitor of histone deacetylase (HDAC) that inhibits the activity of HDAC in Hela cell extracts with 50% inhibition concentration IC50 value of 27 nM. Belinostat has been found to significantly increase the acetylation of histones H3 and H4 and exerts cytotoxicity in a wide range of tumor cell lines. In the treatment of urothelial carcinoma cell lines, belinostat dose-dependently inhibits proliferation in 5637, T24, J82 and RT4 cells with IC50 values of 1.0 μM, 3.5 μM, 6.0 μM and 10 μM respectively; while, in prostate cancer cell lines, it inhibits cancer cell growth with IC50 values ranging from 0.5 to 2.5 μM.

Reference

Michael T Buckley, Joanne Yoon, Herman Yee, Luis Chiriboga, Leonard Liebes, Gulshan Ara, Xiaozhong Qian, Dean F Bajorin, Tung-Tien Sun, Xue-Ru Wu and Iman Osman. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. Journal of Translational Medicine 2007; 5:49

Giovanni Luca Gravina, Francesco Marampon, Ilaria Giusti, Eleonora Carosa, Stefania Di Sante, Enrico Ricevuto, Vincenza Dolo, Vincenzo Tombolini, Emmanuele A Jannini and Claudio Festuccia. Differential effects of PXD101 (belinostat) on androgen-dependent and androgen-independent prostate cancer models. International Journal of Oncology 40: 711-720, 2012

Plumb JA, Finn PW, Williams RJ, Bandara MJ, Romero MR, Watkins CJ, La Thangue NB, Brown R. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8.