MK-2206

MK-2206 is a small molecule allosteric inhibitor of the serine/threonine kinase AKT (also known as protein kinase B). It selectively inhibits all three isoforms of AKT (Akt1, Akt2 and Akt3), which are key components in the PI3K/AKT/mTOR signaling pathway frequently deregulated in many cancers. By inhibiting AKT activity through an allosteric mechanism rather than ATP competition, MK-2206 blocks downstream signaling involved in cell proliferation and survival. It has antineoplastic properties and can induce autophagy. MK-2206 is being investigated primarily as an anticancer agent to overcome resistance to other therapies and enhance chemotherapy efficacy. It has been studied in various solid tumors including breast cancer (notably HER2+ and hormone receptor-negative subtypes), pancreatic cancer, thyroid cancer with PI3K/Akt pathway mutations, non-small cell lung cancer and lymphoma. Clinical trials have demonstrated tolerability with dose-limiting toxicities such as skin rash and stomatitis; it is administered orally. Additionally, preclinical data suggest potential antiviral effects by inducing autophagy that may reduce SARS-CoV-2 replication.

Other names

8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one1,2,4-Triazolo(3,4-f)(1,6)naphthyridin-3(2H)-one, 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-MK-2206 free baseMK2206 free baseMK 2206 free base