MK-2206 free base

Names

[ CAS No. ]:
1032349-93-1

[ Name ]:
MK-2206 free base

[Synonym ]:
UNII-51HZG6MP1K
MK-2206 dihydrochloride

Biological Activity

[Description]:

MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

Akt1:8 nM (IC50)

Akt2:12 nM (IC50)

Akt3:65 nM (IC50)


[References]

[1]. Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.

[2]. Zhao YY, 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.  

[3]. Xing Y, et al. Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/PTEN mutation. Breast Cancer Res. 2019 Jul 5;21(1):78.  

[4]. Agarwal E, et al. Akt inhibitor MK-2206 promotes anti-tumor activity and cell death by modulation of AIF and Ezrin in colorectal cancer. BMC Cancer. 2014 Mar 1;14:145.  

[5]. Zhao YY, 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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C25H21N5O

[ Molecular Weight ]:
407.46700

[ Exact Mass ]:
407.17500

[ PSA ]:
89.33000

[ LogP ]:
5.35530