Pracinostat (SB939)

Catalog No.S1515

Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.

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Pracinostat (SB939) Chemical Structure

Pracinostat (SB939) Chemical Structure
Molecular Weight: 358.48

Validation & Quality Control

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Related Compound Libraries

Pracinostat (SB939) is available in the following compound libraries:

HDAC Inhibitors with Unique Features

Product Information

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Product Description

Biological Activity

Description Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.
Targets HDAC10 [1] HDAC3 [1] HDAC5 [1] HDAC1 [1]

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IC50 40 nM 43 nM 47 nM 49 nM
In vitro SB939 has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. SB939 is a potent inhibitor of HDAC class I isoenzymes, HDAC1, HDAC2, HDAC3 and HDAC8 with the IC50 values ranging from 43 nM to 140 nM. SB939 inhibits HDAC class II isoenzymes , HDAC4, HDAC5, HDAC7, HDAC9 and HDAC10 significantly with the IC50 values ranging from 40 nM to 137 nM, with the exception of HDAC6 which shows IC50 of 1008 nM. It markedly inhibits HDAC11 of the HDAC class IV enzymes with IC50 of 93 nM, but shows no inhibitory activity against SIRT 1 of the class III HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, especially Leukemia cells and cutaneous T-cell Lymphoma cells with IC50 values ranging from 50 nM (H9 cells) to 170 nM (HEL92.1.7 cells). [1]
In vivo Administration of SB939 (25 mg/kg to 100 mg/kg) displays a dose-dependent antitumor efficacy in a xenograft mice model of human colorectal cancer (HCT-116). This is approximately twice as efficacious as SAHA: SB939 causing a tumor growth inhibition of 94% versus 48% by SAHA with both at the maximum tolerated dose. Oral administration of SB939 at a dose of 50 mg/kg or 75 mg/kg in the APCmin genetic mice model of early-stage colon cancer markedly reduces the number of tumors , decreases cumulative hemocult scores and increases hematocrit values more effectively than 5-fluorouracil. [1]
Features A new histone deacetylase inhibitor based on hydroxamic acid, with improved physicochemical, pharmaceutical, and pharmacokinetic properties.

Protocol(Only for Reference)

Kinase Assay: [1]

HDAC enzyme assay All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2 and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software.

Cell Assay: [1]

Cell lines HCT116, A2780, ACHN, MCF7, HL-60, et al.
Concentrations Dissolved in DMSO (stock concentration, 10 mM), final concentrations 1.5 nM to 100 μM
Incubation Time 96 hours
Method Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.

Animal Study: [1]

Animal Models BALB/c nude mice bearing HCT-116 human colon cancer xenografts, Male and APCmin mice
Formulation Dissolved in DMSO and prepared in 0.5% methylcellulose (w/v) and 0.1% Tween-80 in water
Dosages 25, 50, 75, or 100 mg/kg
Administration Oral gavage once daily

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] Novotny-Diermayr V, et al. Mol Cancer Ther, 2010, 9(3), 642-652.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02267278 Recruiting Myeloproliferative Diseases M.D. Anderson Cancer Center|MEI Pharma, Inc. January 2015 Phase 2
NCT02118909 Completed Healthy Volunteers|Non-smokers MEI Pharma, Inc. May 2014 Phase 1
NCT02058784 Completed Healthy Volunteers|Moderate to Heavy Smokers|Non-smokers MEI Pharma, Inc.|Celerion February 2014 Phase 0
NCT01993641 Completed Myelodysplastic Syndrome|MDS MEI Pharma, Inc. December 2013 Phase 2
NCT01912274 Active, not recruiting Acute Myeloid Leukemia MEI Pharma, Inc. October 2013 Phase 2

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Chemical Information

Download Pracinostat (SB939) SDF
Molecular Weight (MW) 358.48
Formula

C20H30N4O2

CAS No. 929016-96-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 72 mg/mL (200.84 mM)
Ethanol 27 mg/mL (75.31 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 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 (E)-3-(2-butyl-1-(2-(diethylamino)ethyl)-1H-benzo[d]imidazol-5-yl)-N-hydroxyacrylamide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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