tcsc0267 Panobinostat

Panobinostat is an oral histone deacetylase (HDAC) inhibitor with a multi-targeted profile.

In Vitro: Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta treatment results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells^[1]. Panobinostat exhibites potent antiproliferative activity in human NSCLC cell lines with the IC₅₀ ranging from 5 to 100 nM^[2].

In Vivo: Panobinosta (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice^[2]. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model^[3].