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[CAS NO. 1032350-13-2]  MK-2206 dihydrochloride

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PRODUCTS SPECIFICATIONS [1032350-13-2]

Catalog
HY-10358
Brand
MCE
CAS
1032350-13-2

DESCRIPTION [1032350-13-2]

Overview

MDLMFCD14584463
Molecular Weight480.39
Molecular FormulaC25H23Cl2N5O
SMILESO=C1N2C(C3=CC(C4=CC=CC=C4)=C(N=C3C=C2)C5=CC=C(C6(N)CCC6)C=C5)=NN1.Cl.Cl

For research use only. We do not sell to patients.

222 Publications Citing Use of MCE


Summary

MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC 50 s of 5 nM, 12 nM, and 65 nM for AKT1 , AKT2 , and AKT3 , respectively. MK-2206 dihydrochloride induces autophagy [1] [3] .


IC50 & Target

Akt1

8 nM (IC 50 )

Akt2

12 nM (IC 50 )

Akt3

65 nM (IC 50 )


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 [3] .
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 [3] .
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 [3] .

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

Cell Proliferation Assay [3]

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 IC 50 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 [3]

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 [3]

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 [3]

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 [3] .
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 [4] .

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 [3]
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

NCT Number Sponsor Condition Start Date Phase
NCT01369849 National Cancer Institute (NCI)
Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia
September 2011 Phase 1|Phase 2
NCT01466868 Centre Leon Berard|National Cancer Institute, France
Diffuse Large B Cell Lymphoma
November 2011 Phase 2
NCT01425879 National Cancer Institute (NCI)
Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma|Recurrent Gallbladder Carcinoma|Stage IV Distal Bile Duct Cancer|Stage IV Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Carcinoma|Unresectable Gallbladder Carcinoma
April 2011 Phase 2

Appearance

Solid


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 : 16.67 mg/mL ( 34.70 mM ; ultrasonic and warming and heat to 70°C)

H 2 O : 3.57 mg/mL ( 7.43 mM ; ultrasonic and warming and heat to 60°C)

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
10 mM 0.2082 mL 1.0408 mL 2.0816 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 25 mg/mL (52.04 mM); Clear solution; Need ultrasonic

  • 2.

    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

  • 3.

    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

* All of the co-solvents are available by MCE.


Synonyms

1,2,4-Triazolo[3,4-f][1,6]naphthyridin-3(2H)-one, 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-, hydrochloride (1:2)
MK 2206 dihydrochloride

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