MK-2206
MK-2206 is an allosteric inhibitor of Akt that prevents translocation of Akt to membranes. MK-2206 exhibits anticancer chemotherapeutic activity in a variety of in vitro cancer models; this compound induces G1-phase cell cycle arrest in hepatocellular carcinoma cells, inhibits cell proliferation in non-small cell lung cancer cells, and inhibits proliferation in medullary thyroid cancer cells. In animal models of nasopharyngeal cancer, MK-2006 inhibits tumor growth.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18945316
| Cas No. |
1032349-77-1 |
|---|---|
| Purity |
≥99% |
| Formula |
C25H22ClN5O |
| Formula Wt. |
443.93 |
| IUPAC Name |
8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;hydrochloride |
| Synonym |
MK-2206 hydrochloride |
| Solubility |
Soluble in DMSO, water with 1 eq. of acid |
| Appearance |
off-white powder |
Zhao YY, Tian Y, Zhang J, et al. Effects of an oral allosteric AKT inhibitor (MK-2206) on human nasopharyngeal cancer in vitro and in vivo. Drug Des Devel Ther. 2014 Oct 10;8:1827-37. pMID: 25336925.
Burke JF, Schlosser L, Harrison AD, et al. MK-2206 Causes Growth Suppression and Reduces Neuroendocrine Tumor Marker Production in Medullary Thyroid Cancer Through Akt Inhibition. Ann Surg Oncol. 2013 Nov;20(12):3862-8. PMID: 23900743.
Jiao P, Zhou YS, Yang JX, et al. MK-2206 induces cell cycle arrest and apoptosis in HepG2 cells and sensitizes TRAIL-mediated cell death. Mol Cell Biochem. 2013 Jun 25. [Epub ahead of print] PMID: 23797319.
Jin R, Nakada M, Teng L, et al. Combination therapy using Notch and Akt inhibitors is effective for suppressing invasion but not proliferation in glioma cells. Neurosci Lett. 2013 Feb 8;534:316-21. PMID: 23262078.
Quayle SN, Lee JY, Cheung LW, et al. Somatic mutations of PIK3R1 promote gliomagenesis. PLoS One. 2012;7(11):e49466. PMID: 23166678.
Iida M, Brand TM, Campbell DA, et al. Targeting AKT with the allosteric AKT inhibitor MK-2206 in non-small cell lung cancer cells with acquired resistance to cetuximab. Cancer Biol Ther. 2013 Jun;14(6):481-91. PMID: 23760490.
Davies BR, Greenwood H, Dudley P, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012 Apr;11(4):873-87. PMID: 22294718.
Cheng Y, Zhang Y, Zhang L, et al. MK-2206, a novel allosteric inhibitor of Akt, synergizes with gefitinib against malignant glioma via modulating both autophagy and apoptosis. Mol Cancer Ther. 2012 Jan;11(1):154-64. PMID: 22057914.
