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MK-2206 (Merck, Whitehouse Station, NJ) is an investigational oral allosteric AKT inhibitor (Appendix Fig A1, online only) with nanomolar potency against purified recombinant human AKT1 (half maximal inhibitory concentration [IC50], 5 nmol/L) and AKT2 enzymes (IC50, 12 nmol/L) but lower potency against human AKT3 (IC50, 65 nmol/L). MK-2206 inhibits phosphorylation at both Thr308 and Ser473 residues of AKT and demonstrates greater than 100-fold selectivity for AKT against 256 other kinases.MK-2206 has in vitro and in vivo antitumor activity as a single agent and enhances the preclinical activity of conventional cytotoxics and other molecular targeted therapies. These promising data led to a phase I dose-escalation study of MK-2206 in patients with advanced solid tumors.
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