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

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Référence HY-10358-10mg

Conditionnement : 10mg

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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.

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MK-2206 dihydrochloride Chemical Structure

CAS No. : 1032350-13-2

This product is a controlled substance and not for sale in your territory.

Based on 348 publication(s) in Google Scholar

Other Forms of MK-2206 dihydrochloride:

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MK-2206 Obtenir un devis

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(26):5250-5264. [Abstract]; Western blotting analysis shows the effect of AKT inhibitor MK2206 (AKT i) and SET7 inhibitor (R)-PFI-2 on the levels of SOX2 proteins. The cells are treated with 1 μM MK2206 for 24 h and 10 μM (R)-PFI-2 for 12 h before being harvested for analysis.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2019 Jan;139(1):71-80. [Abstract]; HEKa (left) and HaCaT (right) cells are seeded in six-cell plates and pretreated with MK2206 for 6 hours, and then stimulated with M5 (2.5 ng/mL) for 48 hours before measuring the protein levels of cyclin D1, Akt, and phosphoAkt by Western blot analysis.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. [Abstract]; Dih10 cells are treated with CDDP (20 μM) in the presence or absence of the Akt inhibitor MK2206 (5 μM).

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 May 8;9(1):1816. [Abstract]; Representative western blot analysis of p-ERK1/2, p-p90 RSK, p-AKT, p-AKT p-PRAS40, p-FOXO1/3a/4, p-GSK3β, p-mTOR, p-p70 S6K, and p-S6 protein in MCF-10A^P and MCF-10A^H1047R cells stably expressing empty vector (EV) or mutant HRAS^Q61R treated with 2 µM MK2206 (AKTi) at different time points.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Oct 3;9(10):1015. [Abstract]; Representative western blot images are showing the LC3, and the phosphorylated and total protein expression of Akt and ERK1/2 after treatment with H₂O₂ in the presence and absence of MK2206 (5 μM) and U0126 (25 μM).

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2018 Nov;39(11):1787-1796. [Abstract]; Effects of LY294002 or AKT siRNA on the levels of total AKT, pAKT, phosphorylated PRAS40 and pMDM2 are examined by Western blot analysis in MCF-7 cells when HBXIP was overexpressed. Effects of MK-2206 or HBXIP siRNA on the levels of total AKT, pAKT, pPRAS40, and pMDM2 are examined by Western blot analysis in MCF-7-HBXIP cells.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):944-955. [Abstract]; Western blotting of Sox2 and b-actin in A549 cells with or without IGF2 treated in the presence or absence of MK-2206.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2018 May 23;10:69. [Abstract]; The expression levels of E-cadherin, vimentin, pan-AKT, p-AKTser473, MMP-2, MMP-7, MMP-9, and actin (control) are detected by Western blot in RAI2 un-expressed and re-expressed RKO and LOVO cells as well as in the control group, shRAI2 knockdown group, and shRAI2 knockdown plus MK2206 treated group.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 May;119(5):3885-3891. [Abstract]; Western blot showed the protein expression of P-gp,MRP1, PTEN, p-AKT, Bax, Bcl-2, and cleaved caspase-3.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2018 Jun;99:43-51. [Abstract]; Western blot analysis of NDRG2, p-ATK, XIAP, E-cadherin and Vimentin in TE-13 cells shows NDRG2 negatively regulates the expressions of AKT, XIAP, E-cadherin and Vimentin proteins.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer. 2018 Jun 14;9(14):2480-2491. [Abstract]; Analysis of indicated proteins in Cry1 silencing osteosarcoma cells after MK-2206 treatment. Data are expressed as the mean±standard deviation.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Radiat Res. 2018 Aug;190(2):204-215. [Abstract]; When 6 Gy irradiation is combined with AKT2 inhibitor MK-2206 treatment, the protein levels in phosphorylated AKT2, mTOR and IKBa are decreased, and the downstream proapoptotic proteins, caspase 3 and caspase 8, are increased.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983. [Abstract]; The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563. [Abstract]; Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Modern Oncology. 2017,25(01):0009-0013.; The related protein expression of Bcl-2, Bax, Caspase-3, PARP, GSK-3β, p65 gene in each intervention group. Western blot assay:1:Control group; 2:MK2206 positive group; 3:0.3g/L Mat; 4: 0.6g/L Mat; 5:1.2g/LMat.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jan 31;8(5):8536-8549. [Abstract]; Western blot analysis of cyclin D1 and cyclin E in OE19 cells treated with the control, BIBR 277 alone, MK-2206 alone, or BIBR 277 combined with MK-2206 for 48 h.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 18;8(29):47642-47654. [Abstract]; Akt/JNK signal pathway is impaired in the inhibition of αMSH on adipocyte inflammation and FoxOs expressions. Mouse adipocytes are pretreated with αMSH and MK-2206, respectively. Relative protein levels of Akt, p-Akt^ser473, JNK, p-JNK^Thr183 with or without MK-2206 (n=3).

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2016 Jul 26;113(30):E4338-47. [Abstract]; HCC1937 cells are treated for 16 h with inhibitors as indicated. Immunoblotting of total cell lysates is performed with antibodies as indicated. Induction of PAR and H2ax phosphorylation (γH2ax) following treatment with inhibitors of pan-PI3K (BKM120, 1.5 μM), PI3Kα (BYL719, 3 μM; PIK75, 0.5 μM), PI3Kβ (TGX221, 30 μM), AZD2281 (5 μM), and inhibitors of AKT (MK2206, 1 μM), SGK (GSK650394, 10 μM), or MAPKK (GSK1120212, 5 nM).

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Graduate School of Arts & Sciences. Harvard University. 2016 Aug.; Mouse embryonic fibroblasts (MEFs) are deprived of Arginine and treated with 2 µM MK2206 for up to 6 hours.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Department of Dental Pharmacology. Okayama University. 2015.; The role of Semaphorin4D in bone invasion by oral cancer.

: MK-2206 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2014 Feb 13;156(4):771-85. [Abstract]; (A) Effects of inhibiting PI3K and Akt in MEFs. Serum starved (16 hr) MEFs are pretreated (30 min) with Wortmannin (100 nM), MK2206 (2 μM) or vehicle (DMSO). Immunoblots of lysates are probed with the indicated antibodies. (B) PTEN null MEFs exhibit constitutive Akt, TSC2 and S6K phosphorylation, which are reversed by the Akt inhibitor MK2206.

Description

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.

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.

Essai clinique

Masse moléculaire

480.39

Formule

C₂₅H₂₃Cl₂N₅O

CAS No.

1032350-13-2

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité

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)

H₂O : 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

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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité
Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureté et documentation

Purity: 99.99%

Select Batch:

Fiche technique (282 KB) SDS (393 KB)

COA (252 KB) HNMR (279 KB) LCMS (89 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.

[2]. 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. [Content Brief]

[3]. Agarwal E, et al. Akt inhibitor MK-2206 promotes anti-tumor activity and cell death by modulation of AIF and Ezrin in colorectal cancer. BMC Cancer. 2014 Mar 1;14:145. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.0816 mL	10.4082 mL	20.8164 mL	52.0410 mL
H₂O / DMSO	5 mM	0.4163 mL	2.0816 mL	4.1633 mL	10.4082 mL
DMSO	10 mM	0.2082 mL	1.0408 mL	2.0816 mL	5.2041 mL
	15 mM	0.1388 mL	0.6939 mL	1.3878 mL	3.4694 mL
	20 mM	0.1041 mL	0.5204 mL	1.0408 mL	2.6021 mL
	25 mM	0.0833 mL	0.4163 mL	0.8327 mL	2.0816 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

MK-2206 dihydrochloride Related Classifications

Stem Cell/Wnt PI3K/Akt/mTOR Autophagy Apoptosis
Organoid Akt Autophagy Apoptosis

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

Référence HY-10358-10mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

Other Forms of MK-2206 dihydrochloride:

Voir tous les produits spécifiques à Isoform Akt:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

MK-2206 dihydrochloride Related Classifications

Keywords:

Vous serez peut-être également intéressé par les produits suivants :

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

Référence HY-10358-10mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

Other Forms of MK-2206 dihydrochloride:

Voir tous les produits spécifiques à Isoform Akt:

MK-2206 dihydrochloride Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

MK-2206 dihydrochloride Related Classifications

Keywords:

Vous serez peut-être également intéressé par les produits suivants :