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1mg |
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5mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Belinostat (formerly PXD-101; PX-105684; NSC-726630; trade name Beleodaq) is a novel, potent and selective HDAC (histone deacetylase) inhibitor with high anticancer activity. The FDA approved it in 2014 for the treatment of peripheral T-cell lymphoma. In a cell-free assay, belinostat inhibits HDACs with an IC50 of 27 nM.
Targets |
HDAC ( IC50 = 27 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Pelletization of subconfluent cultures is achieved by centrifugation at 200 × g for 5 minutes after they are harvested and twice washed in ice cold PBS. The lyse is performed using three freeze (dry ice) thaw (30 °C water bath) cycles after the cell pellet has been resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl]. The supernatant is kept at -80 °C after cell debris is extracted using centrifugation at 1.2 × 104 g for 5 minutes. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK, which corresponds to the 20 NH2-terminal residues) is acetylated by a recombinant protein that uses [3H]acetyl CoA as an acetate source and contains the hypoxanthine-aminopterin-thymidine domain of p300. H4 peptide (100 μg) is combined 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. The mixture is then incubated at 30 °C for 45 minutes. Centrifugation and an hour at 4 °C are used to extract the p300 protein from 20 μL of 50% Ni-agaroase beads. After applying the supernatant to a 2 mL Sephadex G15 column, the flow through is gathered. After adding one milliliter of distilled H2O gently and collecting three drop fractions, this process is repeated until four to five milliliters of distilled H2O are added and approximately forty fractions are collected. The fractions containing the labeled peptide are identified by diluting three microliters of each fraction in two milliliters of scintillation fluid and counting the results in a scintillation counter. These fractions are combined, and a 1 μL sample is measured to determine the radioactivity in each batch of peptides (3-7×103 cpm/μL). The reaction for activity assays is conducted in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] with 2 μL of cell extract and, if applicable, 2 μL of belinostat added. 20 NH2-terminal residues' worth of acetylated histone H4 peptide, or 2 μL of [3H] labeled substrate, is added to initiate the reaction. Samples are incubated for 45 minutes at 37 °C, after which the addition of acetic acid and HCl (0.72 and 0.12 M final concentrations, respectively) stops the reaction. Samples are centrifuged at 1.2× 104 g for 5 minutes after released [3H]acetate is extracted into 750 μL of ethyl acetate. After being transferred to 3 milliliters of scintillation fluid, the upper phase (600 μL) is counted.
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Cell Assay |
After seeding tumor cell lines at a density of 8 × 104 cells/25 cm2 flask in 5 mL of medium, they are incubated for 48 hours. For a full day, cells are subjected to varying concentrations of belinostat (0.016 to 10 μM). After the medium is gone, each flask receives 1 mL of trypsin/EDTA. Following their detachment, the cells are resuspended in 1 mL of medium, and the number of cells from the untreated control flask is recorded. Depending on the cell line, three cells are diluted and plated into 6-cm Petri dishes per flask, with a density of 0.5-2× 103 cells/dish. The drug-treated flasks' cells are diluted and plated similarly to the control flasks. Dishes are incubated at 37 °C for ten to fifteen days. After the cells are fixed in methanol, stained with crystal violet, and rinsed with PBS, colonies containing 50 or more cells are counted. The belinostat concentration needed to lower the number of colonies to 50% of the untreated control cells is known as the IC50, which is used to express sensitivity.
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Animal Protocol |
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References |
Molecular Formula |
C15H14N2O4S
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Molecular Weight |
318.35
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Exact Mass |
318.07
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Elemental Analysis |
C, 56.59; H, 4.43; N, 8.80; O, 20.10; S, 10.07.
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CAS # |
414864-00-9
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Related CAS # |
414864-00-9; 866323-14-0
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Appearance |
White solid powder
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SMILES |
C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)/C=C/C(=O)NO
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InChi Key |
NCNRHFGMJRPRSK-MDZDMXLPSA-N
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InChi Code |
InChI=1S/C15H14N2O4S/c18-15(16-19)10-9-12-5-4-8-14(11-12)22(20,21)17-13-6-2-1-3-7-13/h1-11,17,19H,(H,16,18)/b10-9+
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Chemical Name |
(E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
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Synonyms |
NSC726630; NSC-726630; PX-105684; PXD 101; PXD101; PXD-101; PX105684; PX 105684; NSC-726630; Trade name: Beleodaq
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HS Tariff Code |
2934.99.03.00
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03772925 | Active Recruiting |
Drug: Belinostat Drug: Pevonedistat |
Recurrent Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia |
National Cancer Institute (NCI) |
June 20, 2019 | Phase 1 |
NCT02137759 | Active Recruiting |
Drug: Standard Temozolomide Drug: Belinostat |
Glioblastoma Multiforme of Brain |
Emory University | May 7, 2014 | Phase 2 |
NCT05170334 | Recruiting | Drug: Belinostat Drug: Binimetinib |
Metastatic Uveal Melanoma | H. Lee Moffitt Cancer Center and Research Institute |
December 15, 2021 | Phase 2 |
NCT04703920 | Recruiting | Drug: Talazoparib Drug: Belinostat |
Metastatic Ovarian Carcinoma Metastatic Breast Cancer |
University of Michigan Rogel Cancer Center |
March 4, 2021 | Phase 1 |
NCT02737046 | Recruiting | Drug: Belinostat Drug: Zidovudine |
Adult T-cell Leukemia-Lymphoma ATLL |
University of Miami | December 12, 2016 | Phase 2 |