QTX125 是一种有效且高度选择性的 HDAC6 抑制剂。与其他 HDAC 相比，QTX125 对 HDAC6 具有出色的选择性。QTX125 具有抗肿瘤作用。
QTX125 is a potent and highly selective HDAC6 inhibitor. QTX125 exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects[1].
QTX125 (25-500 nM; 24-48 hours) 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[1]. In MCL cell lines MINO, REC-1, IRM-2 and HBL-2 cells, QTX125 (10 nM, 10 μM, 100 μM) induces dose-dependent hyperacetylation of α-tubulin[1].QTX125 has the strongest growth-inhibitory effect in Burkitt cell lymphoma, follicular lymphoma, and mantle cell lymphoma (MCL)[1].
QTX125 (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[1].
[1]. Montserrat Pérez-Salvia, et al. In vitro and in vivo activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphoma. Haematologica. 2018 Nov;103(11):e537-e540.
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