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| Names | |
|---|---|
| Preferred IUPAC name (2E)-3-{2-Butyl-1-[2-(diethylamino)ethyl]-1H-1,3-benzimidazol-5-yl}-N-hydroxyprop-2-enamide | |
| Other names Pracinostat | |
| Identifiers | |
3D model (JSmol) | |
| ChEBI | |
| ChemSpider | |
| UNII | |
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| Properties | |
| C20H30N4O2 | |
| Molar mass | 358.486 g·mol−1 |
| Density | 1.1±0.1 g/cm3 |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
Pracinostat (SB939) is an orally bioavailable, small-moleculehistone deacetylase (HDAC) inhibitor based onhydroxamic acid with potential anti-tumor activity characterized by favorable physicochemical, pharmaceutical, and pharmacokinetic properties.
Pracinostat selectively inhibits HDAC class I, II, IV without class III and HDAC6 in class IIb,[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 suppressorgenes transcription, and ultimately,apoptosis of tumor cells.[2]
Clinical studies suggests that pracinostat has potential best pharmacokinetic properties when compared to other oral HDAC inhibitors.[3] In March 2014, pracinostat has grantedOrphan Drug foracute myelocytic leukemia (AML) and for the treatment ofT-cell lymphoma by theFood and Drug Administration.
