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Products are for research use only. Not for human use. We do not sell to patients.
(MK-2206 dihydrochloride; MK-2206; MK2206)
MK 2206 Chemical Structure
|Product name: MK 2206|
|Cat. No.: HY-10358|
MK-2206 2Hcl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed.
IC50 value: 8 nM/12 nM/65 nM(Akt1/2/3) 
in vitro: MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins . MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells . MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death .
in vivo: MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg . MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib .
|M.Wt||480.39||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥92mg/mL Water ≥92mg/mL Ethanol ≥1.8mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.0816 mL||10.4082 mL||20.8164 mL|
|5 mM||0.4163 mL||2.0816 mL||4.1633 mL|
|10 mM||0.2082 mL||1.0408 mL||2.0816 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|MK 2206||National Cancer Institute||Gallbladder tumor||31-JAN-13||31-MAY-13||Phase 2||11-OCT-13|
|National Cancer Institute||Biliary cancer||31-JAN-13||31-MAY-13||Phase 2||11-OCT-13|
|National Cancer Institute||Breast tumor||31-JAN-13||31-MAR-16||Phase 2||25-SEP-13|
|National Cancer Institute||Metastatic pancreas cancer||31-AUG-12||Phase 2||17-JUL-13|
|Washington University in St Louis||Breast tumor||30-JUN-13||31-AUG-15||Phase 2||21-JUN-13|
|National Cancer Institute||Metastatic colorectal cancer||31-MAR-13||01-SEP-14||Phase 2||12-SEP-13|
. Hirai H, et al. MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo. Mol Cancer Therapy, 2010, 9(7), 1956-1967.
. Cheng Y, et al. eEF-2 kinase dictates cross-talk between autophagy and apoptosis induced by Akt Inhibition, thereby modulating cytotoxicity of novel Akt inhibitor MK-2206. Cancer Res, 2011, 71(7), 2654-2663.
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