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MK-2206 dihydrochloride

In stock
Catalog No.
A3010
Akt1/2/3 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$120.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$110.00
In stock
50mg
$260.00
In stock
100mg
$400.00
In stock
500mg
$1,500.00
In stock

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Background

MK-2206 dihydrochloride is a selective inhibitor of Akt1/2/3. MK-2206 inhibites the phosphorylation of Thr308 and Ser 473 of Akt. MK-2206 suppresses Akt signalling pathway and promoting cancer cell death as a single agent as well as in combination with other chemotherapeutic agents. MK-2206 enhance the sensitivity to through apoptosis and enhance the sensitivity to rapamycin via reactive oxygen species. Combination of MK-2206 with etoposide or rapamycin significantly increase antitumor growth effect.

References

1. Pant A, Lee II, Lu Z, Rueda BR, Schink J, Kim JJ.Inhibition of AKT with the Orally Active Allosteric AKT Inhibitor, MK-2206, Sensitizes Endometrial Cancer Cells to Progestin.PLoS One. 2012;7(7):e41593. Epub 2012 Jul 24.

2. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. TA Yap, L Yan, A Patnaik, I Fearen.  Journal of Clinical Oncology  2011

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt480.39
Cas No.1032350-13-2
FormulaC25H21N5O.2HCl
SynonymsMK-2206,MK2206,MK 2206
Solubility≥12.01mg/mL in DMSO
Chemical Name8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride
SDFDownload SDF
Canonical SMILESC1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment:[1]

Cell lines

Endometriotic stromal cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

100 nM, 2h

Applications

Inhibiting AKT with MK-2206 or MEK1/2 with U0126 for 24 hours in the absence of R5020 increased total and nuclear PRA and PRB protein levels in OSIS but not in eutopic endometrial stromal cells from disease-free patients from disease-free patients. MK-2206 and R5020 decreased OSIS viability and increased apoptosis. Trends toward decreased volumes of sc grafted endometriosis tissues were demonstrated with MK-2206 and progesterone.

Animal experiment:[1]

Animal models

5-week-old CD-1 nude mice

Dosage form

360 mg/kg/d, 15 days, oral Gavage

Applications

No significant interaction between MK-2206 and progesterone (P=0.628). Trends toward decreased tumor volume were noted with MK-2206 (P=0.077) and progesterone (P=0.087). Treatment with MK-2206 decreased levels of Ki67. Levels of cleaved caspase-3 (CC3) were very low in E and E +P-treated grafts, whereas MK-2206 increased CC3 levels, especially in the presence of P.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Eaton JL1, Unno K, Caraveo M et al. Increased AKT or MEK1/2 activity influences progesterone receptor levels and localization in endometriosis. J Clin Endocrinol Metab. 2013 Dec;98(12):E1871-9.

Biological Activity

Description MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.
Targets Akt1 Akt2 Akt3      
IC50 8 nM 12 nM 65 nM      

Quality Control

Chemical structure

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride

Related Biological Data

MK-2206 dihydrochloride