A potent, orally active allosteric Akt inhibitor with IC50 of 5/12 nM for Akt1/Akt2 respectively; shows 5-fold less potent against human Akt3 (IC50=65 nM); synergistically inhibits cell proliferation of human cancer cell lines in combination with erlotinib or lapatinib in vitro; suppresses the Akt phosphorylation that is induced by carboplatin and gemcitabine.Colon Cancer Phase 2 Clinical(In Vitro):MK-2206 dihydrochloride (MK-2206 (2HCl)) (0-10 μM; 72 and 96 hours) inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner.MK-2206 dihydrochloride (0-10 μM; 24 and 48 hours) results in a dose-dependent increase in the percentage of cells in G0/G1 phase and a concomitant reduction of cell numbers in S phase in CNE-2 and HONE-1 cells.MK-2206 dihydrochloride (0-10 μM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not effect phosphorylation of GSKα/β and AKT.MK-2206 dihydrochloride (0-10 μM; 24 hours) increases the appearance of LC3-II in CNE-2 cells dose-dependently. Microtubule-associated protein 1 LC3 is an essential autophagy protein.(In Vivo):Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice.MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells.
Animal model: Four-to 6-week-old male BALB/c nude mice with CNE-2 xenografts. Dosage: 240 mg/kg and 480 mg/kg. Administration: Oral gavage; 240 mg/kg for three times a week; 480 mg/kg for once a week; for 2 weeks. Result: Both doses inhibited the growth of human CNE-2 xenografts in nude mice.
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