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Submit ReviewMK 2206 dihydrochloride is a potent and selective allosteric Akt inhibitor (IC50 values are 5 nM, 12 nM, and 65 nM for Akt1, Akt2, and Akt3, respectively). MK 2206 requires the Pleckstrin homology domain for its activity, and exhibits no inhibitory activity in a panel of 250 tested protein kinases. MK 2206 induces growth inhibition of different cancer cell lines (IC50 in the range 3.4 and 28.6 μmol/L) and enhances antitumor efficacy of a range of standard chemotherapeutics. It synergistically inhibits cell proliferation of human lung and breast cancer cells in combination with Erlotinib (Cat. No. 7194) by suppressing both the Ras/Erk and PI 3-K pathways in vitro and in vivo. MK 2206 can be used to block the IL-22 - Akt signaling pathway for studying paneth cell differentiation.
M. Wt | 480.39 |
Formula | C25H21N5O.2HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1032350-13-2 |
PubChem ID | 46930998 |
InChI Key | HWUHTJIKQZZBRA-UHFFFAOYSA-N |
Smiles | O=C1NN=C2C3=C(C=CN12)N=C(C4=CC=C(C5(CCC5)N)C=C4)C(C6=CC=CC=C6)=C3.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 24.02 | 50 |
The following data is based on the product molecular weight 480.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.16 mL | 20.82 mL | 41.63 mL |
2.5 mM | 0.83 mL | 4.16 mL | 8.33 mL |
5 mM | 0.42 mL | 2.08 mL | 4.16 mL |
25 mM | 0.08 mL | 0.42 mL | 0.83 mL |
References are publications that support the biological activity of the product.
He et al (2022) Optimized human intestinal organoid model reveals interleukin-22-dependency of paneth cell formation. Cell Stem Cell 29 1333 PMID: 36002022
Hirai et al (2010) 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. 9 1956 PMID: 20571069
Li et al (2009) Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. AACR Annual Meeting 69
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