QTX125 TFA

• CAT Number: I045537
• CAS Number: 2989537-78-0
• Molecular Formula: C25H20F3N3O7
• Molecular Weight: 531.44
• Purity: ≥95%
• Synonyms: 3-(furan-3-yl)-N-[[4-(hydroxycarbamoyl)phenyl]methyl]-5-(4-hydroxyphenyl)-1H-pyrrole-2-carboxamide;2,2,2-trifluoroacetic acid
• InChI: InChI=1S/C23H19N3O5.C2HF3O2/c27-18-7-5-15(6-8-18)20-11-19(17-9-10-31-13-17)21(25-20)23(29)24-12-14-1-3-16(4-2-14)22(28)26-30;3-2(4,5)1(6)7/h1-11,13,25,27,30H,12H2,(H,24,29)(H,26,28);(H,6,7)
• InChIKey: YVRBCQZCFZYITL-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1CNC(=O)C2=C(C=C(N2)C3=CC=C(C=C3)O)C4=COC=C4)C(=O)NO.C(=O)(C(F)(F)F)O

QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects[1].
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[1]. ?
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[1].?
QTX125 TFA has the strongest growth-inhibitory effect in Burkitt cell lymphoma, follicular lymphoma, and mantle cell lymphoma (MCL)[1].
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[1].

Reference

[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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