A pan-Pim kinase inhibitor
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).1 It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.1 It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.2,3
1.Keeton, E.K., McEachern, K., Dillman, K.S., et al.AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemiaBlood123(6)905-913(2014) 2.Harada, M., Benito, J., Yamamaoto, S., et al.The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppressionOncotarget6(35)37930-37947(2015) 3.Iqbal, A., Eckerdt, F., Bell, J., et al.Targeting of glioblastoma cell lines and glioma stem cells by combined PIM kinase and PI3K-p110α inhibitionOncotarget7(22)33192-33201(2016)
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