MK-2206 (free base)

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].

Product Specifications

CAS Number

[1032349-93-1]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Akt; Apoptosis; Autophagy; Organoid

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mk-2206.html

Solubility

10 mM in DMSO

Smiles

O=C1N2C(C3=CC(C4=CC=CC=C4)=C(C(C=C5)=CC=C5C6(CCC6)N)N=C3C=C2)=NN1

Molecular Formula

C25H21N5O

Molecular Weight

407.47

Precautions

P261-P280-P302+P352

References & Citations

[1]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.|[2]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.|[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]Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.|[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.