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MK-2206

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MK-2206
Names
Preferred IUPAC name 8--9-phenyltriazolo naphthyridin-3(2H)-one
Identifiers
CAS Number
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
ECHA InfoCard 100.207.435 Edit this at Wikidata
EC Number
  • 682-246-4
PubChem CID
UNII
CompTox Dashboard (EPA)
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 407.477 g·mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). Infobox references
Chemical compound

MK-2206 is a drug candidate being investigated to help treat cancer. Its chemical formula is C25H21N5O. It acts as an allosteric AKT inhibitor.

It is a highly selective inhibitor of pan-Akt, namely, of all three Akt isoforms Akt1, Akt2, and Akt3.

It is intended to be used with other cancer therapies that advanced tumours may become resistant to.

Clinical trials

2011: A phase 1 clinical trial of MK-2206 alone has reported it was well tolerated.
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.
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.
As of August 2017 31 phase II clinical trials are registered, many completed. e.g. in colorectal cancer, breast cancer, and many others.

MK-2206 and COVID-19

Data shown in a study preprint suggest that SARS-CoV-2 infection decreases cellular autophagy and that MK-2206, which induces autophagy, reduced virus replication by up to 88% in vitro. The study's authors propose that MK-2206 should be tested in clinical trials as a potential treatment for COVID-19.

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. Yap TA, Yan L, Patnaik A, Fearen I, Olmos D, Papadopoulos K, et al. (December 2011). "First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors". Journal of Clinical Oncology. 29 (35): 4688–4695. doi:10.1200/JCO.2011.35.5263. PMID 22025163.
  5. Novel Agents are Targeting Drivers of TNBC - Several drug candidates in I-SPY2 have 'graduated' to later-phase studies. June 2016
  6. MK-2206 phase=2 trials
  7. Gassen NC, Papies J, Bajaj T, Emanuel J, Dethloff F, Chua RL, et al. (June 2021). "SARS-CoV-2-mediated dysregulation of metabolism and autophagy uncovers host-targeting antivirals". Nature Communications. 12 (1): 3818. doi:10.1038/s41467-021-24007-w. PMC 8217552. PMID 34155207.
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