QTX125

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

QTX125 (QTX-125) 是一种新型有效的选择性 HDAC6 抑制剂，与其他 HDAC 相比具有出色的选择性。

QTX125 (QTX-125) is a novel potent, selective HDAC6 inhibitor, displays excellent selectivity over other HDACs; strongly reduces cell viability with IC50 values of 0.120 and 0.182 uM in two primary samples obtained from patients with MCL; causes cell-growth inhibition and programmed cell death in association with increased levels of acetylated α-tubulin, also antitumoral effect is particularly evident in MCL models, both in culture and in vivo, surpassing the efficacy of currently available HDAC6 inhibitors.

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. 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.QTX125 has the strongest growth-inhibitory effect in Burkitt cell lymphoma, follicular lymphoma, and mantle cell lymphoma (MCL). Apoptosis Analysis Cell Line:MINO, REC-1, IRM-2 and HBL-2 cells Concentration:25 nM, 50 nM, 100 nM, 500 nM Incubation Time:24 hours, 48 hours Result:Inhibited annexin V/propidium iodide double staining.Western Blot Analysis Cell Line:MINO, REC-1, IRM-2 and HBL-2 cells Concentration:25 nM, 50 nM, 100 nM, 500 nM Incubation Time:24 hours Result:Inhibited the cleavage of caspase-9, caspase-8, caspase-3, and PARP.

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. Animal Model:Nude mice bearing REC-1 or MINO cells Dosage:60 mg/kg Administration:Intraperitoneal administration; daily dosing for 5 days; for 4 weeks Result:Inhibited tumor growth in REC-1 or MINO cells xenografted in nude mice.

QTX 125 | QTX-125

Cell Cycle/DNA Damage

HDAC

HDAC

——

——

1279698-31-5

417.421

C23H19N3O5

>98% (HPLC)

——

O=C(C1=C(C2=COC=C2)C=C(C3=CC=C(O)C=C3)N1)NCC4=CC=C(C(NO)=O)C=C4

3-(3-furyl)-N-{4-[(hydroxyamino)carbonyl]benzyl}-5-(4-hydroxyphenyl)-1H-pyrrole2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years