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SB939

Cat. No. M1778
SB939 Structure
Synonym:

Pracinostat

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 210  USD210 In stock
50mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

SB939 is a novel potent and orally active histone deacetylase with high tumor exposure and efficacy in mouse models of colorectal cancer. The IC50 value for HDAC1 is 52 nM. In vitro, SB939 inhibits class I, II and IV HDACs, with no effects on other zinc binding enzymes, and shows significant antiproliferative activity against a wide variety of tumor cell lines. It has very favorable pharmacokinetic properties after oral dosing in mice, with >4-fold increased bioavailability and 3.3-fold increased half-life over suberoylanilide hydroxamic acid (SAHA).

Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2010). Figure 1. SB939
Method Western blots
Cell Lines HCT-116 colon cancer cells
Concentrations 0.25 to 1 μmol/L
Incubation Time 24 h
Results No signal for acH3 could be detected in vehicle-treated cells, whereas SB939 in concentrations of 0.125 μmol/L and above induced acH3 and the acetylation of α-tubulin after 24 h of treatment. Concentrations of 0.25 μmol/L and above led to decreased retinoblastoma serine phosphorylation on S807/811, an increase of the cyclin-dependant kinase inhibitor p21Cip/WAF.
Protocol (for reference only)
Cell Experiment
Cell lines Colo205, HCT-116, A2780, PC3, DU145, MCF7, NCI-H460, HEP3B cells line
Preparation method Cell Proliferation Assay
Cells were seeded in 96-well plates at a predetermined optimal density, in the log growth phase, and rested for 24 h (adherent cells) or 2 h (suspension cells), respectively, before treatment with SB939. All experiments were done in triplicates for 96 h, with 1% solvent, using either the CyQUANT Cell proliferation assay kit (Invitrogen Corp.) for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit (Promega Corp.) for suspension cells, according to the manufacturer's instructions, in a total volume of 100 μL with SB939 concentrations from 100 μmol/L to 1.5 nmol/L in nine serial dilution steps. IC50 were determined using the XLfit software (IDBS).
Concentrations 0~100 μ M
Incubation time 96 h
Animal Experiment
Animal models HCT-116 Xenograft Mouse Model(Female BALB/c nude mice)
Formulation 0.5% methylcellulose (w/v) and 0.1% Tween-80 in water (oral) or normal saline(i.v)
Dosages once daily for 21 d with 25, 50, 75, or 100 mg/kg
Administration oral
Chemical Information
Molecular Weight 358.48
Formula C20H30N4O2
CAS Number 929016-96-6
Solubility (25°C) DMSO 65 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Novotny-Diermayr V, et al. Blood Cancer J. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML.

[2] Sumanadasa SD, et al. Antimicrob Agents Chemother. Antimalarial activity of the anticancer histone deacetylase inhibitor SB939.

[3] Jayaraman R, et al. Drug Metab Dispos. Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics.

[4] Wang H, et al. J Med Chem. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.

[5] Novotny-Diermayr V, et al. Mol Cancer Ther. Pharmacodynamic evaluation of the target efficacy of SB939, an oral HDAC inhibitor with selectivity for tumor tissue.

[6] Yong WP, et al. Ann Oncol. Phase I and pharmacodynamic study of an orally administered novel inhibitor of histone deacetylases, SB939, in patients with refractory solid malignancies.

[7] Novotny-Diermayr V, et al. Mol Cancer Ther. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer.

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Keywords: SB939, Pracinostat supplier, HDAC, inhibitors, activators


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