|
Biological Activity:
An orally potent and highly selective non-ATP comeptitive allosteric Akt inhibitor that has nanomolar IC50 values and broad preclinicl anti-tumor activities.
References: online
H Hirai et al. MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo. Mol. Cancer Ther. 2010, 9(7), 1956-1967. [online]
AW Tolcher et al. A phase I study of MK-2206, an oral potent allosteric Akt inhibitor (Akti), in patients (pts) with advanced solid tumor (ST). J. Clin. Oncol. 27:15s, 2009 (suppl; abstr 3503). [online]
R Liu et al. The Akt-Specific Inhibitor MK2206 Selectively Inhibits Thyroid Cancer Cells Harboring Mutations That Can Activate the PI3K/Akt Pathway. J. Clin. Endocrinol. Metab. 2011, 96(4), E577-E585. [online]
Chemical Name: 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-8,9-dihydro-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one
|