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SB939

Cat. No. M1778

SB939 Structure

Synonym: Pracinostat

Size Price Availability Quantity
10mg USD 300 In stock
50mg USD 715 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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).

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 358.48
Formula C20H30N4O2
CAS Number 929016-96-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML.
Novotny-Diermayr V, et al. Blood Cancer J. 2012 May;2(5):e69. PMID: 22829971.

Antimalarial activity of the anticancer histone deacetylase inhibitor SB939.
Sumanadasa SD, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3849-56. PMID: 22508312.

Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics.
Jayaraman R, et al. Drug Metab Dispos. 2011 Dec;39(12):2219-32. PMID: 21873472.

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.
Wang H, et al. J Med Chem. 2011 Jul 14;54(13):4694-720. PMID: 21634430.

Pharmacodynamic evaluation of the target efficacy of SB939, an oral HDAC inhibitor with selectivity for tumor tissue.
Novotny-Diermayr V, et al. Mol Cancer Ther. 2011 Jul;10(7):1207-17. PMID: 21586629.

Phase I and pharmacodynamic study of an orally administered novel inhibitor of histone deacetylases, SB939, in patients with refractory solid malignancies.
Yong WP, et al. Ann Oncol. 2011 Nov;22(11):2516-22. PMID: 21385886.

SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer.
Novotny-Diermayr V, et al. Mol Cancer Ther. 2010 Mar;9(3):642-52. PMID: 20197387.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB939, Pracinostat supplier, HDAC, inhibitors

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