Loading... Please wait...

Categories

Our Newsletter


MK-2206 | Akt1/Akt2/Akt3 inhibitor

  • MK-2206.jpg
  • MK-2206, 400x400px, png

Price:
$129.00
Catalog #:
C6220-5
Quantity:


Product Description

MK-2206 is an orally bioavailable allosteric quinolinotriazolone inhibitor of the serine/threonine protein kinase Akt. It is selectively potent for Akt1, Akt2, and Akt3 at 5 nM, 12 nM, and 65 nM, respectively. MK-2206 inhibits auto-phosphorylation of Akt1/2 at position T308 and S473.

Combination studies with EGFR inhibitors (e.g. erlotinib and lapatinib) in cancer cell lines have shown synergistic effects in a dose-dependent manner [1], inhibiting both PI3K and Ras/Erk pathways. Recent studies indicate that breast cancer cell lines with PTEN loss and/or PIK3CA mutations were also more sensitive to MK-2206 [3], and that targeting eEF-2 kinase in conjunction with Akt can also enhance its antitumor effect [2].


Technical information:

Chemical Formula:   C25H21N5O.2HCl
CAS #:   1032350-13-2
Molecular Weight:   480.39
Purity:   >98%
Appearance:   Bright Yellow
Chemical Name:   8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one
Solubility:   Up to 20 mM in DMSO
Synonyms:   MK-2206, MK 2206, MK2206

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Hirai et al., MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo. Mol Cancer Ther, 2010, 9(7), 1956. Pubmed ID: 20571069
2. Liu et al., Roles of eEF-2 kinase in cancer. Chin Med J 2012 125(16), 2908-2913 Pubmed ID: 22932089
3. Gonzalez-Angulo et al., Defining biomarkers to predict sensitivity to PI3K/Akt/mTOR pathway inhibitors in breast cancer. Cancer Treatment Rev 2012, in press.

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Add to Wish List

Click the button below to add the MK-2206 | Akt1/Akt2/Akt3 inhibitor to your wish list.

You Recently Viewed...