CX-6258 hydrochloride hydrate is a potent and kinase-selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM, and 16 nM for Pim-1, Pim-2, and Pim-3, respectively. It is intended for research use only and not for sale to patients.
- Potent and kinase selective pan-Pim kinases inhibitor.
- Inhibits the phosphorylation of pro-survival proteins Bad and 4E-BP1 at specific Pim kinase sites (S112, S65, and T37/46 respectively).
- Diminishes steady-state levels of ectopic NKX3.1 in PC3 cells.
- Reduces NKX3.1 half-life.
- Exhibits robust in vivo efficacy in two Pim kinases driven tumor models, showing dose-dependent tumor growth inhibition (TGI) of 45% at 50 mg/kg and 75% at 100 mg/kg in MV-4-11 xenograft models in nude mice.