MK 2206 2HCL
MK-2206
CAS: 1032350-13-2
Molecular Formula: C25H21N5O
MK 2206 2HCL - Names and Identifiers
MK 2206 2HCL - Physico-chemical Properties
| Molecular Formula | C25H21N5O |
| Molar Mass | 407.46714 |
| Melting Point | >255°C (dec.) |
| Solubility | Soluble in DMSO (up to 10 mg/ml with warming) |
| Appearance | Yellow powder. |
| Color | Yellow |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Use | MK-2206 2HCl is a highly selective Akt1/2/3 inhibitor with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activity against 250 other protein kinases. |
| In vitro study | MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits the autophosphorylation of The threonine 308 site and the serine 473 site of Akt. In addition, MK-2206 prevents phosphorylation of Akt-regulated downstream signaling molecules, including TSC2, PRAS40, and ribosomal S6 proteins. MK-2206 inhibits Ras wild-type cell lines (e. G., NCI-H358, NCI-H23, NCI-H1299, and Calu-6) more effectively than Ras mutant cell lines (e. G., A431, HCC827, and NCI-H292). The combination of MK-2206 and cytotoxic agents such as erlotinib and lapatinib MK-2206 also show synergistic effects on lung NCI-H460 tumor cells or ovarian A2780 tumor cells. |
| In vivo study | MK-2206 combined with these cytotoxic agents act on NCI-H292 xenograft tumors and MK-2206 exhibit very potent anticancer activity. In ovarian cancer A2780 transplanted tumor, 240mg of MK-2206 per kilogram of animal weight can inhibit more than 70% of Akt1/2 phosphorylation at threonine 308 site and serine 473 site, this resulted in a tumor growth inhibition rate of 60%. |
MK 2206 2HCL - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.082 ml | 10.408 ml | 20.816 ml |
| 5 mM | 0.416 ml | 2.082 ml | 4.163 ml |
| 10 mM | 0.208 ml | 1.041 ml | 2.082 ml |
| 5 mM | 0.042 ml | 0.208 ml | 0.416 ml |
Last Update：2024-01-02 23:10:35
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