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MK-2206 dihydrochloride

Catalog No. T1952 CAS 1032350-13-2

Synonyms: MK-2206 2HCl

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

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MK-2206 dihydrochloride Chemical Structure

MK-2206 dihydrochloride, CAS 1032350-13-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 30.00
5 mg	In stock	$ 47.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 97.00
50 mg	In stock	$ 147.00
100 mg	In stock	$ 228.00
200 mg	In stock	$ 372.00
500 mg	In stock	$ 615.00
1 mL * 10 mM (in DMSO)	In stock	$ 51.00

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Purity: 99.91%

Purity: 99.69%

Purity: 99.59%

Purity: 99.228%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.
Targets&IC50	Akt3:65 nM (cell free), Akt2:12 nM (cell free), Akt1:8 nM (cell free)
In vitro	METHODS: Fourteen tumor cells were treated with MK-2206 dihydrochloride for 72 h. Cell viability was measured by CellTiter-Glo assay. RESULTS: MK-2206 dihydrochloride inhibited the growth of tumor cells with IC50 ranging from 0.1 to 28.6 μmol/L. [1] METHODS: Human nasopharyngeal carcinoma cell lines CNE-2 and HONE-1 were treated with MK-2206 dihydrochloride (0.625-10 μM) for 24-48 h, and the cell cycle was detected by Flow Cytometry. RESULTS: MK-2206 dihydrochloride caused a dose-dependent increase in the percentage of cells in G0/G1 phase and a decrease in the number of cells in S phase.MK-2206 dihydrochloride induced cell cycle arrest in G1 phase. MK-2206 dihydrochloride induces cell cycle arrest in the G1 phase. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, MK-2206 dihydrochloride (120 mg/kg three times per week or 360 mg/kg once per week, 30% Captisol) and erlotinib (50 mg/kg five times per week, 0.5% methylcellulose + 0.1% Tween 80) were orally administered to CD1 mice bearing human lung cancer tumor NCI-H292 for two weeks. RESULTS: Three-times-weekly MK-2206 monotherapy was ineffective, and the once-weekly regimen mediated only moderate antitumor efficacy. Although erlotinib alone mediated significant tumor growth inhibition, combination therapy with MK-2206 significantly enhanced its antitumor efficacy, including tumor regression. [1] METHODS: To assay antitumor activity in vivo, MK-2206 dihydrochloride (120 mg/kg in 30% captisol) was administered by gavage to NSG mice bearing human endometrial cancer tumors twice a week for three weeks. RESULTS: MK-2206 dihydrochloride treatment resulted in significant inhibition of the growth of three different types and grades of PDX tumors. [3]
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].
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].

Synonyms	MK-2206 2HCl
Molecular Weight	480.39
Formula	C25H23Cl2N5O
CAS No.	1032350-13-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 7.5 mg/mL (15.61 mM)

References and Literature

1. 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. 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. 3. Winder A, et al. The allosteric AKT inhibitor, MK2206, decreases tumor growth and invasion in patient derived xenografts of endometrial cancer. Cancer Biol Ther. 2017 Dec 2;18(12):958-964. 4. Jin J, Zhao Y, Guo W, et al. Thiocoraline mediates drug resistance in MCF-7 cells via PI3K/Akt/BCRP signaling pathway[J]. Cytotechnology. 2019 Feb;71(1):401-409. 5. He J, Zhang A, Song Z, et al. The resistant effect of SIRT1 in oxidative stress-induced senescence of rat nucleus pulposus cell is regulated by Akt-FoxO1 pathway[J]. Bioscience reports. 2019 May 10;39(5). pii: BSR20190112. 6. Lv W, Huan M, Yang W, et al. Snail promotes prostate cancer migration by facilitating SPOP ubiquitination and degradation[J]. Biochemical and Biophysical Research Communications. 2020, 529(3): 799-804. 7. Lv, Wei, et al. Snail promotes prostate cancer migration by facilitating SPOP ubiquitination and degradation. Biochemical and Biophysical Research Communications . 529.3 (2020): 799-804. 8. Li Z, Zhou Z, Wu X, et al. LMP1 promotes nasopharyngeal carcinoma metastasis through NTRK2-mediated anoikis resistance[J]. American journal of cancer research . 2020, 10(7): 2083. 9. Zhou C, Du J, Zhao L, et al. GLI1 reduces drug sensitivity by regulating cell cycle through PI3K/AKT/GSK3/CDK pathway in acute myeloid leukemia[J]. Cell Death & Disease. 2021, 12(3): 1-14. 10. Zhang L, Zhou Q, Qiu Q, et al. CircPLEKHM3 acts as a tumor suppressor through regulation of the miR-9/BRCA1/DNAJB6/KLF4/AKT1 axis in ovarian cancer[J]. Molecular Cancer. 2019, 18(1): 1-19.

Citations

1. Jiang Y, Zhao X, Chen J, et al.PM2. 5 induces cardiac malformations via PI3K/akt2/mTORC1 signaling pathway in zebrafish larvae.Environmental Pollution.2023: 121306. 2. Zhao W, Xu C, Peng L, et al.cAMP/PKA signaling promotes AKT deactivation by reducing CIP2A expression, thereby facilitating decidualization.Molecular and Cellular Endocrinology.2023: 111946. 3. Mavrogonatou E, Angelopoulou M, Rizou S V, et al. Activation of the JNKs/ATM-p53 axis is indispensable for the cytoprotection of dermal fibroblasts exposed to UVB radiation. Cell death & disease. 2022, 13(7): 1-14. 4. Hou X, Liu Q, Gao Y, et al. Mesencephalic astrocyte-derived neurotrophic factor reprograms macrophages to ameliorate acetaminophen-induced acute liver injury via p38 MAPK pathway. Cell Death & Disease. 2022, 13(2): 1-13. 5. Zhang P, Zhang J, Quan H, et al. Effects of butein on human osteosarcoma cell proliferation, apoptosis, and autophagy through oxidative stress. Human & Experimental Toxicology. 2022, 41: 09603271221074346. 6. Lv W, Huan M, Yang W, et al. Snail promotes prostate cancer migration by facilitating SPOP ubiquitination and degradation. Biochemical and Biophysical Research Communications. 2020, 529(3): 799-804 7. Li Z, Zhou Z, Wu X, et al. LMP1 promotes nasopharyngeal carcinoma metastasis through NTRK2-mediated anoikis resistance. American journal of cancer research. 2020, 10(7): 2083. 8. Zhou C, Du J, Zhao L, et al. GLI1 reduces drug sensitivity by regulating cell cycle through PI3K/AKT/GSK3/CDK pathway in acute myeloid leukemia. Cell Death & Disease. 2021, 12(3): 1-14. 9. Liu Y, Wang J, Chen J, et al. Upregulation of miR-520c-3p via Hepatitis B Virus Drives Hepatocellular Migration and Invasion through the PTEN/AKT/NF-κB Signaling Pathway. Molecular Therapy-Nucleic Acids. 2022 10. Zhang L, Zhou Q, Qiu Q, et al. CircPLEKHM3 acts as a tumor suppressor through regulation of the miR-9/BRCA1/DNAJB6/KLF4/AKT1 axis in ovarian cancer. Molecular Cancer. 2019, 18(1): 1-19

11. Zhang H, Xia P, Liu J, et al. ATIC inhibits autophagy in hepatocellular cancer through the AKT/FOXO3 pathway and serves as a prognostic signature for modeling patient survival. International Journal of Biological Sciences. 2021, 17(15): 4442-4458. 12. He J, Zhang A, Song Z, et al. The resistant effect of SIRT1 in oxidative stress-induced senescence of rat nucleus pulposus cell is regulated by Akt-FoxO1 pathway. Bioscience Reports. 2019 May 10;39(5). pii: BSR20190112 13. Jin J, Zhao Y, Guo W, et al. Thiocoraline mediates drug resistance in MCF-7 cells via PI3K/Akt/BCRP signaling pathway. Cytotechnology. 2019 Feb;71(1):401-409.

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Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Kinase Inhibitor Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Ovarian Cancer Compound Library Orally Active Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

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