| Size | Price | |
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| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg |
MK-2206 (MK2206) is a novel and potent Akt inhibitor with anticancer activities. It inhibits AKT with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively.
| ln Vitro |
In a dose- and time-dependent manner, MK-2206 (0-10 μM; 72 and 96 hours) suppresses the growth of the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1[3]. For CNE-2 and HONE-1 cells, MK-2206 (0-10 μM; 24 and 48 hours) causes a dose-dependent rise in the proportion of G0/G1 phase cells and a corresponding decrease in S phase cell numbers[3]. The phosphorylation levels of S6 and PRAS40 are attenuated in a dose-dependent manner by MK-2206 (0-10 μM; 24 hours). GSKα/β and AKT phosphorylation is unaffected by MK-2206.[/3]. In CNE-2 cells, MK -2206 (0-10 μM; 24 hours) dose-dependently promotes the appearance of LC3-II. Autophagy requires the crucial protein microtubule-associated protein 1 (LC3)[3].
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| ln Vivo |
Human CNE-2 xenograft development in nude mice can be inhibited by MK-2206 at both oral gavage doses (480 mg/kg once a week and 240 mg/kg three times a week; for two weeks). In mice, no further apparent harm is noted[3]. When given orally, MK-2206 (120 mg/kg on alternate days) dramatically reduces the formation of tumors in 3–5 week old athymic nude mice harboring GEO colon cancer cells[4].
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| Cell Assay |
Cell Proliferation Assay[3]
Cell Types: The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 Tested Concentrations: 0.08, 0.16, 0.31, 0.63, 1.25, 2.5, 5, 10 μM Incubation Duration: 72 and 96 hrs (hours) Experimental Results: At 72 and 96 hrs (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[3] Cell Types: CNE-2 and HONE-1 cells Tested Concentrations: 0.625, 1.25, 2.5, 5, 10 μM Incubation Duration: 24 or 48 hrs (hours) Experimental Results: Induced cell cycle arrest at G1 in a dose-dependent manner. Western Blot Analysis[3] Cell Types: SUNE-1 and CNE-2 cells Tested Concentrations: 0.625, 1.25, 2.5, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited phosphorylation of AKT downstream targets. Cell Autophagy Assay[3] Cell Types: CNE-2 cells Tested Concentrations: 0.625, 1.25, 2.5, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced autophagy. |
| Animal Protocol |
Animal/Disease Models: Four - to 6weeks old male BALB/c nude mice with CNE-2 xenografts[3]
Doses: 240 mg/kg and 480 mg/kg Route of Administration: po (oral gavage); 240 mg/kg for three times a week; 480 mg/ kg for once a week; for 2 weeks Experimental Results: Both doses inhibited the growth of human CNE-2 xenografts in nude mice. |
| References |
[1]. Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.
[2]. Xing Y, et al. Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/PTEN mutation. Breast Cancer Res. 2019 Jul 5;21(1):78. [3]. 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. [4]. 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. |
| Molecular Formula |
C₂₅H₂₂CLN₅O
|
|---|---|
| Molecular Weight |
443.93
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| CAS # |
1032349-77-1
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| Related CAS # |
MK-2206 dihydrochloride;1032350-13-2;MK-2206 free base;1032349-93-1
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| SMILES |
O=C1NN=C2C3C=C(C4C=CC=CC=4)C(C4C=CC(=CC=4)C4(CCC4)N)=NC=3C=CN21
|
| Synonyms |
MK2206 MK 2206
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2526 mL | 11.2630 mL | 22.5261 mL | |
| 5 mM | 0.4505 mL | 2.2526 mL | 4.5052 mL | |
| 10 mM | 0.2253 mL | 1.1263 mL | 2.2526 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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