MK-2206 is an orally bioavailable allosteric quinolinotriazolone inhibitor of the serine/threonine protein kinase Akt. It is selectively potent for Akt1, Akt2, and Akt3 at 5 nM, 12 nM, and 65 nM, respectively. MK-2206 inhibits auto-phosphorylation of Akt1/2 at position T308 and S473.
Combination studies with EGFR inhibitors (e.g. erlotinib and lapatinib) in cancer cell lines have shown synergistic effects in a dose-dependent manner [1], inhibiting both PI3K and Ras/Erk pathways. Recent studies indicate that breast cancer cell lines with PTEN loss and/or PIK3CA mutations were also more sensitive to MK-2206 [3], and that targeting eEF-2 kinase in conjunction with Akt can also enhance its antitumor effect [2].
Technical information:
Chemical Formula: | C25H21N5O.2HCl | |
CAS #: | 1032350-13-2 | |
Molecular Weight: | 480.39 | |
Purity: | >98% | |
Appearance: | Bright Yellow | |
Chemical Name: | 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one | |
Solubility: | Up to 20 mM in DMSO | |
Synonyms: | MK-2206, MK 2206, MK2206 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Hirai 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 Ther, 2010, 9(7), 1956. Pubmed ID: 20571069 |
2. | Liu et al., Roles of eEF-2 kinase in cancer. Chin Med J 2012 125(16), 2908-2913 Pubmed ID: 22932089 |
3. | Gonzalez-Angulo et al., Defining biomarkers to predict sensitivity to PI3K/Akt/mTOR pathway inhibitors in breast cancer. Cancer Treatment Rev 2012, in press. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.