PIM-Kinase Inhibitor X, CX-6258

An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC₅₀ = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; K_i = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC₈₀ >500 nM). Shown to arrest the proliferation of several human cancer cells (IC₅₀ = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser¹¹², 4E-BP1-Ser⁶⁵ and Thr^37/46 with an IC₅₀ of ~ 1.0 µM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380 ) and paclitaxel (Cat. No. 580555 ) toxicity in PC3 cells.

Cell permeable: yes

Primary Target
PIM Kimases

Reversible: yes

Secondary Target
Flt3

Target IC₅₀: 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3

Packaged under inert gas

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 135.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)