MK-2206
 | |
| Names | |
|---|---|
| IUPAC name
8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one | |
| Identifiers | |
| 3D model (Jmol) | Interactive image |
| ChemSpider | 24658140 |
| PubChem | 24964624 |
| |
| |
| Properties | |
| C25H21N5O | |
| Molar mass | 407.48 g·mol−1 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
MK-2206 is a drug candidate being investigated to help treat cancer. Its chemical formula is C25H21N5O.[1] It acts as an allosteric AKT inhibitor.[2]
It is a highly selective inhibitor of pan-Akt, namely, of all three Akt isoforms Akt1, Akt2, and Akt3.[1]
It is intended to be used with other cancer therapies that advanced tumours may become resistant to.[3]
Clinical trials
2011: A phase 1 clinical trial of MK-2206 alone has reported it was well tolerated.[4]
2014: A phase 1 clinical trial of MK-2206 with a variety of other agents in 72 patients with advanced cancer reported acceptable side-effects.[3]
2016: MK-2206 is one of the treatments in the I-SPY2 Adaptive clinical trial for breast cancer that had been selected for later stage trials.[5]
References
- 1 2 MK-2206 dihydrochloride (CAS 1032350-13-2) inc structure diagram
- ↑ MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo. Hirai et al. 2010
- 1 2 A trial of MK-2206 with chemotherapy or erlotinib for advanced cancer
- ↑ First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors.
- ↑ Novel Agents are Targeting Drivers of TNBC - Several drug candidates in I-SPY2 have 'graduated' to later-phase studies. June 2016
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