Panobinostat-d4 (hydrochloride) is intended for use as an internal standard for the quantification of panobinostat by GC- or LC-MS. Panobinostat is a pan-inhibitor of histone deacetylases (HDACs; Kis = 0.6-31 nM for HDAC1-11).1 It inhibits growth in a panel of 37 human or mouse lung cancer cell lines, including small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), and mesothelioma cancer cells (IC50s = 4-175, 5-310, and 5-470 nM, respectively), but not NCI H661 mouse NSCLC cells (IC50 = >800 nM).2 Panobinostat (20 mg/kg, i.p.) induces tumor regression in BK-T and RG-1 SCLC mouse xenograft models.
1.Wang, H., Yu, N., Chen, D., et al.Discovery of (2E)-3-{2-butyl-1-[2-diethylamino)ethyl]-1H-benzamidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profileJ. Med. Chem.54(13)4694-4720(2011) 2.Crisanti, M.C., Wallace, A.F., Kapoor, V., et al.The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancerMol. Cancer Ther.8(8)2221-2231(2009)