MK-2206

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
ChemSpider	24658140
Jmol interactive 3D	Image
PubChem	24964624
InChI InChI=1S/C25H21N5O/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31) Key: ULDXWLCXEDXJGE-UHFFFAOYSA-N InChI=1/C25H21N5O/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31) Key: ULDXWLCXEDXJGE-UHFFFAOYAX
SMILES C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N
Properties
Chemical formula	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]

References

1. MK-2206 dihydrochloride (CAS 1032350-13-2) inc structure diagram
2. 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
3. A trial of MK-2206 with chemotherapy or erlotinib for advanced cancer
4. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors.