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> MK-2206 (dihydrochloride) [1032350-13-2]

MK-2206 (dihydrochloride) [1032350-13-2]

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Cat# HY-10358-10mg

Size : 10mg

Brand : MedChemExpress

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Description

MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy[1][2].

IC50 & Target[1]

Akt1

8 nM (IC50)

Akt2

12 nM (IC50)

Akt3

65 nM (IC50)

In Vitro

MK-2206 dihydrochloride (MK-2206 (2HCl)) (0-10 μM; 72 and 96 hours) inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner[1].
MK-2206 dihydrochloride (0-10 μM; 24 and 48 hours) results in a dose-dependent increase in the percentage of cells in G0/G1 phase and a concomitant reduction of cell numbers in S phase in CNE-2 and HONE-1 cells[2].
MK-2206 dihydrochloride (0-10 μM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not effect phosphorylation of GSKα/β and AKT[2].
MK-2206 dihydrochloride (0-10 μM; 24 hours) increases the appearance of LC3-II in CNE-2 cells dose-dependently. Microtubule-associated protein 1 LC3 is an essential autophagy protein[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MK-2206 dihydrochloride Related Antibodies

Cell Proliferation Assay[2]

Cell Line: The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1
Concentration: 0.08, 0.16, 0.31, 0.63, 1.25, 2.5, 5, 10 μM
Incubation Time: 72 and 96 hours
Result: At 72 and 96 hours, the IC50 values in CNE-1, CNE-2, and HONE-1 cell lines were 3-5 μM, and in SUNE-1, they were less than 1 μM.

Cell Cycle Analysis[2]

Cell Line: CNE-2 and HONE-1 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 or 48 hours
Result: Induced cell cycle arrest at G1 in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: SUNE-1 and CNE-2 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Inhibited phosphorylation of AKT downstream targets.

Cell Autophagy Assay[2]

Cell Line: CNE-2 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Induced autophagy.
In Vivo

Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice[2].
MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts[2]
Dosage: 240 mg/kg and 480 mg/kg
Administration: Oral gavage; 240 mg/kg for three times a week; 480 mg/kg for once a week; for 2 weeks
Result: Both doses inhibited the growth of human CNE-2 xenografts in nude mice.
Clinical Trial
Molecular Weight

480.39

Formula

C25H23Cl2N5O
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1N2C(C3=CC(C4=CC=CC=C4)=C(N=C3C=C2)C5=CC=C(C6(N)CCC6)C=C5)=NN1.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (26.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0816 mL 10.4082 mL 20.8164 mL
5 mM 0.4163 mL 2.0816 mL 4.1633 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (3.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (3.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  20% SBE-β-CD in Saline

    Solubility: 25 mg/mL (52.04 mM); Clear solution; Need ultrasonic
Purity & Documentation
References

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