Pracinostat
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| Names | |
|---|---|
| IUPAC name
(E)-3-(2-Butyl-1-(2-(diethylamino)ethyl)-1H-benzo[d]imidazol-5-yl)-N-hydroxyacrylamide | |
| Other names
Pracinostat | |
| Identifiers | |
| 929016-96-6 | |
| 3D model (Jmol) | Interactive image |
| ChemSpider | 25027185 |
| PubChem | 49855250 |
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| |
| Properties | |
| C20H30N4O2 | |
| Molar mass | 358.49 g·mol−1 |
| Density | 1.1±0.1 g/cm3 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
Pracinostat (SB939) is an orally bioavailable, small-molecule histone deacetylase (HDAC) inhibitor based on hydroxamic acid with potential anti-tumor activity characterized by favorable physicochemical, pharmaceutical, and pharmacokinetic properties.
Activity
Pracinostat selectively inhibits HDAC class I,II,IV without class III and HDAC6 in class IV,[1] but has no effect on other Zn-binding enzymes, receptors, and ion channels. It accumulates in tumor cells and exerts a continuous inhibition to histone deacetylase,resulting in acetylated histones accumulation, chromatin remodeling, tumor suppressor genes transcription, and ultimately, apoptosis of tumor cells.[2]
Clinical medication
Clinical studies suggests that pracinostat has potential best pharmacokinetic properties when compared to other oral HDAC inhibitors.[3] In March 2014, pracinostat has granted Orphan Drug for acute myelocytic leukemia (AML) and for the treatment of T-cell lymphoma by the Food and Drug Administration.
References
- ↑ "In vitro enzyme activity of SB939 and SAHA". 22 Aug 2014.
- ↑ "The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML". Blood Cancer Journal. doi:10.1038/bcj.2012.14.
- ↑ Veronica Novotny-Diermayr; et al. (March 9, 2010). "SB939, a Novel Potent and Orally Active Histone Deacetylase Inhibitor with High Tumor Exposure and Efficacy in Mouse Models of Colorectal Cancer". Mol Cancer Ther. doi:10.1158/1535-7163.MCT-09-0689.