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AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML.
AZD1208 suppresses the growth of MOLM 16 and KG 1 xenograft tumors in vivo in a dosedependent manner. Furthermore, AZD1208 leads to potent inhibition of colony development of primary AML cells from bone marrow aspirates and downregulates the phosphorylation of PIM goals. AZD1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of PIM1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture.