QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.In Vitro: QTX125 (25-500 nM; 24-48 hours) TFA treatment induces the subsequent apoptosis demonstrated by annexin V/propidium iodide double staining and the cleavage of caspase-9, caspase-8, caspase-3, and PARP.
In MCL cell lines MINO, REC-1, IRM-2 and HBL-2 cells, QTX125 TFA (10 nM, 10 μM, 100 μM) induces dose-dependent hyperacetylation of α-tubulin.
QTX125 TFA has the strongest growth-inhibitory effect in Burkitt cell lymphoma, follicular lymphoma, and mantle cell lymphoma (MCL).In Vivo: QTX125 TFA (60 mg/kg; i.p.; daily dosing for 5 days; for 4 weeks) treatment inhibits tumor growth in REC-1 or MINO cells xenografted in nude mice.