Resminostat (4SC-201) is a novel, orally bioavailable histone deacetylase (HDAC) inhibitor for the treatment of cancers. Resminostat inhibited proliferation and induced G0/G1 cell cycle arrest in 3 out of 4 MM cell lines accompanied with decreased levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21 at 1 micromol/l. Resminostat (4SC-201) induces hyperacetylation of histone H4 in MM cells. Low micromolar concentrations of resminostat (RAS2410) abrogated cell growth and strongly induced apoptosis (IC50=2.5-3 micromol/l in 3 out of 4 MM cell lines) in MM cell lines as well as primary MM cells. Resminostat decreased phosphorylation of 4E-BP1 and p70S6k indicating an interference with Akt pathway signalling. Resminostat treatment resulted in increased protein levels of Bim and Bax and decreased levels of Bcl-xL.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells.
Mandl-Weber S, et al. Br J Haematol. 2010 May;149(4):518-28. PMID: 20201941.
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