PTG-0861
Names
[ CAS No. ]:
2494082-34-5
[ Name ]:
PTG-0861
Biological Activity
[Description]:
PTG-0861 (JG-265) is a novel potent, selective HDAC6 inhibitor with IC50 of 5.92 nM, >36-fold selectivity over other HDACs.PTG-0861 (JG-265) displays HDAC6 cellular target engagement with EC50 of 0.59 uM (ELISA), has in vitro and cellular selectivity superior to HDAC6-selective inhibitor citarinostat (ACY-241).PTG-0861 (JG-265) demonstrates potency against several blood cancer cell lines (e.g. MV4-11, MM1S), whilst showing limited cytotoxicity against non-malignant cells and CD-1 mice.PTG-0861 (JG-265) exihibits promising in vitro pharmacokinetics achieved with good safety profile in cells and in vivo.
[References]
1. Justyna M Gawel, et al. Eur J Med Chem. 2020 Sep 1;201:112411.
Chemical & Physical Properties
[ Molecular Formula ]:
C15H9F5N2O3
[ Molecular Weight ]:
360.24
Related Compounds
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