MK-2206/[email protected]

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MK-2206 is an orally active allosteric Akt inhibitor that is under development for the treatment of solid tumors. MK-2206 is a highly potent and selective Akt inhibitor. It is equally potent toward purified recombinant human Akt1 (IC50, 5 nmol/L) and Akt2 enzyme (IC50, 12 nmol/L) and approximately 5-fold less potent against human Akt3 (IC50, 65 nmol/L; ref. 24). In the present report, we describe the combination effects of MK-2206 with various anticancer drugs, including docetaxel, carboplatin, gemcitabine, 5-fluorouracil (5-FU), doxorubicin, camptothecin, and RTK inhibitors such as lapatinib and erlotinib.

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM). In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines. At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.