MK-2206 dihydrochlorideMK-2206 dihydrochloride
MedChemExpress (MCE)
HY-10358
1032350-13-2
MK-2206 (2HCl)
99.93%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
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[1]. 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[2]. 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[2]. 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[2].
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[2]. 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[3].
Akt1 8 nM (IC50) Akt2 12 nM (IC50) Akt3 65 nM (IC50)
| | | |
| | | | | |
[1]. Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.
[2]. Zhao YY, et al. Effects of an oral allosteric AKT inhibitor (MK-2206) on human nasopharyngeal cancer in vitro and in vivo. Drug Des Devel Ther. 2014 Oct 10
8:1827-37. [Content Brief]
[3]. Agarwal E, et al. Akt inhibitor MK-2206 promotes anti-tumor activity and cell death by modulation of AIF and Ezrin in colorectal cancer. BMC Cancer. 2014 Mar 1
14:145. [Content Brief]