MK 2206 dihydrochloride

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Description: Potent and selective allosteric Akt1, Akt2 and Akt3 inhibitor
Chemical Name: 8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Pathways (1)

Biological Activity for MK 2206 dihydrochloride

MK 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.

Technical Data for MK 2206 dihydrochloride

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.

Solubility Data for MK 2206 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.02 50

Preparing Stock Solutions for MK 2206 dihydrochloride

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for MK 2206 dihydrochloride

References for MK 2206 dihydrochloride

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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Citations for MK 2206 dihydrochloride

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Pathways for MK 2206 dihydrochloride

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.