Name: Pracinostat (SB939)
Brand: Selleck Chemicals
SKU: S1515
Rating: 5 (24 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Other HDAC Inhibitors	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.17 μM	24119555
NCI-H460 cells	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.22 μM	24119555
HCT116 cells	Proliferation assay	48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.24 μM	24119555
MDA-MB-435 cells	Proliferation assay	48 h	Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.48 μM	24119555
OVCAR5 cells	Proliferation assay	48 h	Antiproliferative activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=0.61 μM	24119555
HepG2	Antimalarial assay		Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells, IC50 = 0.15 μM.	24904967
HepG2	Antiplasmodial assay	53 hrs	Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method, IC50 = 0.15 μM.	28241112
Sf9	Function assay	2 hrs	Inhibition of recombinant human HDAC-2 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM.	ChEMBL
HEK293-F	Function assay	2 hrs	Inhibition of recombinant human HDAC-8 expressed in HEK293-F cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM.	ChEMBL
Sf9	Function assay	2 hrs	Inhibition of recombinant human HDAC-1 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM.	ChEMBL
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	358.48	Formula	C₂₀H₃₀N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	929016-96-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)C=CC(=O)NO

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (200.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 27 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	A new histone deacetylase inhibitor based on hydroxamic acid, with improved physicochemical, pharmaceutical, and pharmacokinetic properties.
Targets/IC₅₀/Ki	HDAC10 (Cell-free assay) 40 nM HDAC3 (Cell-free assay) 43 nM HDAC5 (Cell-free assay) 47 nM HDAC1 (Cell-free assay) 49 nM HDAC4 (Cell-free assay) 56 nM HDAC9 (Cell-free assay) 70 nM HDAC11 (Cell-free assay) 93 nM HDAC2 (Cell-free assay) 96 nM HDAC7 (Cell-free assay) 137 nM HDAC8 (Cell-free assay) 140 nM HDAC6 (Cell-free assay) 1.008 μM
In vitro	Pracinostat (SB939) has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. This compound 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. It 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. This chemical shows significant antiproliferative activity against a wide variety of tumour cell lines, especially Leukaemia cells and cutaneous T-cell Lymphoma cells with IC50 values ranging from 50 nM (H9 cells) to 170 nM (HEL92.1.7 cells).
Kinase Assay	HDAC enzyme assay
Kinase 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 this compound, 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.
In vivo	Administration of this compound (25 mg/kg to 100 mg/kg) displays a dose-dependent anti-tumour efficacy in a xenograft mice model of human colorectal cancer (HCT-116). This is approximately twice as efficacious as SAHA: this chemical causing a tumour growth inhibition of 94% versus 48% by SAHA with both at the maximum tolerated dose. Oral administration of this agent at a dose of 50 mg/kg or 75 mg/kg in the APC^min genetic mice model of early-stage colon cancer markedly reduces the number of tumours, decreases cumulative hemoccult scores and increases haematocrit values more effectively.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20197387/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-JAK2 / JAK2 / p-STAT5 / STAT5 / p-FLT3 / FLT3		22829971

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02118909	Completed	Healthy Volunteers\|Non-smokers	Helsinn Healthcare SA	May 2014	Phase 1
NCT02058784	Completed	Healthy Volunteers\|Moderate to Heavy Smokers\|Non-smokers	Helsinn Healthcare SA\|Celerion	February 2014	Early Phase 1
NCT01112384	Completed	Metastatic Sarcoma	NCIC Clinical Trials Group\|S*BIO\|Canadian Cancer Trials Group	October 21 2010	Phase 2
NCT00741234	Completed	Solid Tumors\|Hematologic Malignancies\|Myelodysplastic Syndrome	S*BIO	April 2007	Phase 1

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Pracinostat (SB939) HDAC inhibitor

Chemical Structure

Molecular Weight: 358.48