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MK-2206 dihydrochloride
Catalog No.
A3010
Akt1/2/3 inhibitor
Featured Products
MK-2206 dihydrochloride is a selective inhibitor of Akt1/2/3. MK-2206 inhibites the phosphorylation of Thr308 and Ser 473 of Akt. MK-2206 suppresses Akt signalling pathway and promoting cancer cell death as a single agent as well as in combination with other chemotherapeutic agents. MK-2206 enhance the sensitivity to through apoptosis and enhance the sensitivity to rapamycin via reactive oxygen species. Combination of MK-2206 with etoposide or rapamycin significantly increase antitumor growth effect.
References
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2. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. TA Yap, L Yan, A Patnaik, I Fearen.? Journal of Clinical Oncology? 2011
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 480.39 |
| Cas No. | 1032350-13-2 |
| Formula | C25H21N5O·2HCl |
| Synonyms | MK-2206,MK2206,MK 2206 |
| Solubility | insoluble in EtOH; ≥12.01 mg/mL in DMSO; ≥2.74 mg/mL in H2O with ultrasonic |
| Chemical Name | 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Endometriotic stromal cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
100 nM, 2h |
|
Applications |
Inhibiting AKT with MK-2206 or MEK1/2 with U0126 for 24 hours in the absence of R5020 increased total and nuclear PRA and PRB protein levels in OSIS but not in eutopic endometrial stromal cells from disease-free patients from disease-free patients. MK-2206 and R5020 decreased OSIS viability and increased apoptosis. Trends toward decreased volumes of sc grafted endometriosis tissues were demonstrated with MK-2206 and progesterone. |
| Animal experiment:[1] | |
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Animal models |
5-week-old CD-1 nude mice |
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Dosage form |
360 mg/kg/d, 15 days, oral Gavage |
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Applications |
No significant interaction between MK-2206 and progesterone (P=0.628). Trends toward decreased tumor volume were noted with MK-2206 (P=0.077) and progesterone (P=0.087). Treatment with MK-2206 decreased levels of Ki67. Levels of cleaved caspase-3 (CC3) were very low in E and E +P-treated grafts, whereas MK-2206 increased CC3 levels, especially in the presence of P. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Eaton JL1, Unno K, Caraveo M et al. Increased AKT or MEK1/2 activity influences progesterone receptor levels and localization in endometriosis. J Clin Endocrinol Metab. 2013 Dec;98(12):E1871-9. |
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| Description | MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively. | |||||
| Targets | Akt1 | Akt2 | Akt3 | |||
| IC50 | 8 nM | 12 nM | 65 nM | |||
Quality Control & MSDS
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