AZD1208 is a potent and selective, ATP-competitive pan-Pim kinase inhibitor with IC50 of 0.4/5.0/1.9 nM for Pim-1/2/3, respectively. AZD1208 has Ki values of 0.1 nM for Pim-1, 1.92 nM for Pim-2, and 0.4 nM for Pim-3. AZD1208 inhibits AML cell-line growth and can induce cell-cycle arrest and apoptosis, accompanied by a dose-dependent reduction in phosphorylation of Bcl-2 antagonist of cell death, 4EBP1, p70S6K, and S6. AZD1208 potently inhibits the level of pBAD with IC50 of 10 nM for Pim-1, 151 nM for Pim-2, and 102 nM for Pim-3in U2-OS cells. AZD1208 (10 mg/kg or 30 mg/kg) inhibits the growth of MOLM-16 and KG-1a xenograft tumors in vivo.
