Resminostat
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Names | |
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IUPAC name
(2E)-3-[1-({4-[(Dimethylamino)methyl]phenyl}sulfonyl)-1H-pyrrol-3-yl]-N-hydroxyacrylamide | |
Other names
RAS2410; Resminostat 4SC-201 | |
Identifiers | |
864814-88-0 | |
ChemSpider | 9784710 |
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Jmol-3D images | Image |
PubChem | 11609955 |
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Properties | |
Molecular formula |
C16H19N3O4S |
Molar mass | 349.40 g·mol−1 |
Density | 1.282 g/cm3 |
Except where noted otherwise, data is given for materials in their standard state (at 25 °C (77 °F), 100 kPa) | |
Infobox references | |
Resminostat (RAS2410) is an orally bioavailable inhibitor of histone deacetylases (HDACs), of which inhibitors are antineoplastic agents.[1]
In 2011, the German drug maker 4SC was granted orphan drug designation for resminostat by the Food and Drug Administration for the treatment of hepatocellular cancer/HCC.[2]
Mechanism
Resminostat restrains the phosphorylation of 4E-BP1 and p70S6k, indicating an disturbance with Akt signalling pathway.The treatment of resminostat leads to a drop of Bim and Bax protein level and Bcl-xL level.[3]
As with other inhibitors such as pracinostat, the inhibition of HDACs by resminostat results in an accumulation of highly acetylated histones, followed by an abduction of chromatin remodeling, inhibition of tumor suppressor genes transcription and cell division, and finally tumor cell apoptosis.
References
- ↑ "Biological activity of resminostat in selleck chemicals research". selleck.
- ↑ "4SC's Anti-Cancer Drug Resminostat achieves Median Overall Survival of 8.0 Months in Second-Line Advanced Liver Cancer (HCC) Patients". September 2012.
- ↑ Brunetto AT et al. (1 Oct 2013). "First-in-human, pharmacokinetic and pharmacodynamic phase I study of Resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors." 19 (19). pp. 5494–504. doi:10.1158/1078-0432.CCR-13-0735.