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Formula | C25H21N5O.2HCl |
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Molecular Weight | 480.39 | CAS No. | 1032350-13-2 | ||||
Solubility (25°C)* | In vitro | DMSO | 25 mg/mL (52.04 mM) | ||||
Water | 2 mg/mL (4.16 mM) | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2. | ||||||
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Targets |
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In vitro | MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. [1] MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents in lung NCI-H460 or ovarian A2780 tumor cells. [2] MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death. [3] |
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In vivo | MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg. [1] MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination. [2] |
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Features | The first allosteric small molecule inhibitor of Akt to enter clinical development. |
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Data from [Data independently produced by Nat Commun, 2015, 6:6943]
Data from [Data independently produced by Leukemia, 2015, 29(1), 169-76]
Data from [Data independently produced by J Exp Med, 2014, 211(9), 1741-58]
Data from [Cancer Cell, 2013, 24, 766-76]
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The Cortisol Effect on the NO/cGMP Pathway [ Int J Mol Sci, 2025, 26(4)1421] | PubMed: 40003888 |
Sotorasib resistance triggers epithelial-mesenchymal transition and activates AKT and P38-mediated signaling [ Front Mol Biosci, 2025, 12:1537523] | PubMed: 39950162 |
Insights into the Mode of Action of Novel Morpholinated Curcumin Derivatives Exhibiting Potent Antitumor Activity in Bladder Cancer Cells In Vitro [ Molecules, 2025, 30(2)295] | PubMed: 39860164 |
CD20 and CD19 promote proliferation driven by the IgM-TLR9-L265P MyD88 complex [ Int Immunol, 2025, dxaf004] | PubMed: 39868594 |
Low-Dose Perifosine, a Phase II Phospholipid Akt Inhibitor, Selectively Sensitizes Drug-Resistant ABCB1-Overexpressing Cancer Cells [ Biomol Ther (Seoul), 2025, 33(1):170-181] | PubMed: 39632683 |
A novel DNA repair protein, N-Myc downstream regulated gene 1 (NDRG1), links stromal tumour microenvironment to chemoresistance [ bioRxiv, 2025, 2025.01.22.634323] | PubMed: 39896456 |
ROR2 Regulates Cellular Plasticity in Pancreatic Neoplasia and Adenocarcinoma [ Cancer Discov, 2024, 14(11):2162-2182] | PubMed: 38975886 |
The pro-oncogenic noncanonical activity of a RAS•GTP:RanGAP1 complex facilitates nuclear protein export [ Nat Cancer, 2024, ] | PubMed: 39528835 |
mTORC2-driven chromatin cGAS mediates chemoresistance through epigenetic reprogramming in colorectal cancer [ Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0] | PubMed: 39080411 |
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