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Purity: ≥98%
Pracinostat (formerly SB-939) is a novel, potent and orally bioavailable pan-HDAC (histone deacetylase) inhibitor with potential anticancer activity. As opposed to class III HDACs, it shows comparatively higher selectivity (more than 1000-fold) for class I, class II, and class IV HDACs. Prostate carcinomas, colon cancer, ovarian cancer, acute myeloid leukemia (AML), B cell lymphoma, and other cancer cell lines are among those against which it exhibits strong anti-proliferative activity in vitro. In order to treat acute myelocytic leukemia (AML) and T-cell lymphoma, pracinostat was given FDA Orphan Drug status in March 2014.
| Targets |
HDAC10 ( IC50 = 40 nM ); HDAC3 ( IC50 = 43 nM ); HDAC5 ( IC50 = 47 nM ); HDAC1 ( IC50 = 49 nM ); HDAC4 ( IC50 = 56 nM ); HDAC9 ( IC50 = 70 nM ); HDAC11 ( IC50 = 93 nM ); HDAC2 ( IC50 = 96 nM ); HDAC7 ( IC50 = 137 nM ); HDAC8 ( IC50 = 140 nM ); HDAC6 ( IC50 = 1008 nM ); MBLAC2 ( IC50 < 10 nM )
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| Enzyme Assay |
All recombinant HDAC enzymes are expressed in S*BIO through cloning, except for SIRT1. The assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2, and 1 mg/mL BSA), various concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM are all included in the reaction mix, which has a total reaction volume of 33 μL. The mixture is then incubated at room temperature for two hours. After adding 16 μL of Flour de LysTM developer, incubate for an extra 10 minutes. With a microplate reader, the light emission is measured at 460 nm. To generate IC50 values, use the XLfit software.
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| Cell Assay |
Prior to treating with SB939, cells are seeded at a predefined optimal density in 96-well plates during the log growth phase, and they are allowed to rest for either 24 hours (for adherent cells) or 2 hours (for suspension cells). All the experiments are conducted in triplicates for 96 hours using 1% solvent. For adherent cells, the CyQUANT Cell Proliferation Assay Kit is used, and for suspension cells, the CellTiter96 Aqueous One solution cell proliferation kit. The total volume used in the experiments is 100 μL, and the concentrations of SB939 are diluted nine times in serial order to get from 100 μM to 1.5 nM. The XLfit software is utilized to ascertain the IC50 [1].
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| References |
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| Molecular Formula |
C20H30N4O2
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| Molecular Weight |
358.48
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| Exact Mass |
358.24
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| Elemental Analysis |
C, 67.01; H, 8.44; N, 15.63; O, 8.93
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| CAS # |
929016-96-6
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| Appearance |
White solid powder
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| SMILES |
CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)/C=C/C(=O)NO
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| InChi Key |
JHDKZFFAIZKUCU-ZRDIBKRKSA-N
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| InChi Code |
InChI=1S/C20H30N4O2/c1-4-7-8-19-21-17-15-16(10-12-20(25)22-26)9-11-18(17)24(19)14-13-23(5-2)6-3/h9-12,15,26H,4-8,13-14H2,1-3H3,(H,22,25)/b12-10+
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| Chemical Name |
(E)-3-[2-butyl-1-[2-(diethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide
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| Synonyms |
SB939; SB-939; SB 939
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7896 mL | 13.9478 mL | 27.8956 mL | |
| 5 mM | 0.5579 mL | 2.7896 mL | 5.5791 mL | |
| 10 mM | 0.2790 mL | 1.3948 mL | 2.7896 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 |
| NCT03495934 | Completed | Drug: pracinostat | Healthy Subjects | Helsinn Healthcare SA | February 8, 2018 | Phase 1 |
| NCT01112384 | Completed | Drug: SB939 | Metastatic Sarcoma | NCIC Clinical Trials Group | October 21, 2010 | Phase 2 |
| NCT01184274 | Completed | Drug: SB939 | Leukemia Solid Tumours |
NCIC Clinical Trials Group | October 1, 2010 | Phase 1 |
| NCT01200498 | Completed | Drug: SB939 | Myeloproliferative Disorders | M.D. Anderson Cancer Center | November 2010 | Phase 2 |
| NCT01075308 | Completed | Drug: HDAC inhibitor SB939 | Prostate Cancer | NCIC Clinical Trials Group | June 28, 2010 | Phase 2 |
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