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Cytoskeletal Signaling Akt MK-2206 dihydrochloride

MK-2206 dihydrochloride

Catalog No. T1952   CAS 1032350-13-2
Synonyms: MK-2206 2HCl

MK-2206 is a highly specific inhibitor of Akt1/2/3 (IC50: 8/12/65 nM in cell-free assays) and no effect on the activities of 250 other protein kinases.

MK-2206 dihydrochloride, CAS 1032350-13-2
Pack Size Availability Price/USD Quantity
2 mg In stock 40.00
5 mg In stock 57.00
10 mg In stock 75.00
25 mg In stock 140.00
50 mg In stock 175.00
100 mg In stock 255.00
200 mg In stock 438.00
1 mL * 10 mM (in DMSO) In stock 57.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description MK-2206 is a highly specific inhibitor of Akt1/2/3 (IC50: 8/12/65 nM in cell-free assays) and no effect on the activities of 250 other protein kinases.
Targets&IC50 Akt1 :ic50 8 nM (cell free),   Akt2 :ic50 12 nM (cell free),   Akt3 :ic50 65 nM (cell free),  
Kinase Assay Akt kinases assay: Akt kinases are assayed by a GSK-derived biotinylated peptide substrate. The extent of peptide phosphorylation is determined by Homogeneous Time Resolved Fluorescence (HTRF) using a lanthanide chelate (Lance)-coupled monoclonal antibody specific for the phosphopeptide in combination with a streptavidin-linked allophycocyanin (SA-APC) fluorophore which will bind to the biotin moiety on the peptide. When the Lance and APC are in proximity, a non-radiative energy transfer takes place from the Lance to the APC, followed by emission of light from APC at 655 nm. Working Solution: 100X protease inhibitor cocktail (PIC): 1mg/mL benzamidine, 0.5 mg/mL pepstatin, 0.5 mg/mL leupeptin, 0.5 mg/mL aprotinin; 10X assay buffer: 500 mM HEPES, pH7.5, 1% PEG, 16.6 mM EDTA, 1 mM EGTA, 1% BSA, 20 mM 9-glycerol phosphate; Quench buffer 50 mM HEPES pH 7.3, 16.6 mM EDTA, 0.1% BSA, 0.1% Triton X-100, 0.17 nM labeled monoclonal antibody, 0.0067 mg/mL SA-APC; ATP/MgCl2 working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, active Akt; Peptide working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, 2 TM GSK biotinylated peptide. The reaction is assembled by adding 16 µL of ATP/MgCl2 working solution to the appropriate wells. MK-2206 or vehicle (1.0 µL) is added followed by 10 µL of peptide working solution. The reaction is started by adding 13 μL of the enzyme working solution and mixing. The reaction is allowed to proceed for 50 min and then stopped by the addition of 60 µL HTRF quench buffer. The stopped reactions are incubated at room temperature for at least 30 min and then read in the instrument.
Cell Research
Cells were seeded at a density of 2 to 3 × 103 per well in 96-well plates. Twenty-four hours after plating, varying concentrations of the drug, either as a single agent or in combination, were added to the wells. Cell proliferation was determined by using the CellTiter-Glo assay at 72 or 96 hours after dosing. The nature of the drug interaction was evaluated by using the combination index (CI) according to the method of Chou and Talalay. A commercial software package was obtained from Calcusyn. In combination with docetaxel, we tested three treatment sequences: (a) MK-2206 followed by docetaxel—cells were exposed to MK-2206 for 24 hours, and then after washout of MK-2206, cells were treated with docetaxel for an additional 72 hours; (b) docetaxel followed by MK-2206—cells were exposed to docetaxel for 24 hours, and then after washout of docetaxel, cells were treated with MK-2206 for an additional 72 hours; and (c) concurrent treatment—cells were exposed to both MK-2206 and docetaxel for 72 hours [2].
Cell lines: A431, HCC827, NCI-H292, NCI-H358, NCI-H23, NCI-H1299, Calu-6 and NCI-H460 cells
Animal Research
When the mean tumor size reached 0.13 cm3 for the SK-OV-3 or 0.2 cm3 for the NCI-H292, HCC70, PC-3, and NCI-H460 models, the mice were randomized into control and treatment groups with approximately equivalent ranges of tumor volume between groups (n = 5 animals per group). The following vehicles were used to dose the compounds: 30% Captisol (Cydex) for MK-2206; 0.5% methylcellulose + 0.1% Tween 80 for erlotinib; distilled water for lapatinib; 0.73% ethanol in saline for docetaxel; and saline for carboplatin and gemcitabine. The control group received vehicle only. Tumor volume was measured with calipers twice a week. Animal body weight and physical signs were monitored during the experiments. Tumor volume was calculated, taking length to be the longest diameter across the tumor and width to be the perpendicular diameter, by using the following formula: (length × width)2 × 0.5. Relative tumor volume was assessed by dividing the tumor volume on different observation days with the starting tumor volume. Statistical significance was evaluated by using the two-way repeated ANOVA test followed by Dunnett's test or an unpaired t-test [2].
Animal Model: SK-OV-3, NCI-H292, HCC70, PC-3, and NCI-H460 models in CD1-nude mice
Synonyms MK-2206 2HCl
Purity 99.91%
Molecular Weight 480.39
Formula C25H23Cl2N5O
CAS No. 1032350-13-2

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 12 mg/mL (25 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

15% Captisol: 17 mg/mL

Citations

References and Literature
1. Yan L. MK-2206: a potent oral allosteric AKT inhibitor. AACR Annual Meeting 2009: Abstract Number: DDT01-1. 2. 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 Ther. 2010 Jul;9(7):1956-67. 3. 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.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Autophagy Compound Library PI3K-AKT-mTOR Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library

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