MK-2206 dihydrochloride

Short Summary : Akt1/2/3 inhibitor

Category : PI3K/Akt/mTOR Signaling|Akt

Purity : 0.9944

CAS Number : 1032350-13-2

Formula : C25H21N5O.2HCl

Molecular Weight : 480.39

SMILE : C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl

Solubility : >12mg/mL in DMSO

Storage : Store at -20°C

Description : MK-2206 dihydrochloride is a selective inhibitor of Akt1/2/3. MK-2206 inhibites the phosphorylation of Thr308 and Ser 473 of Akt. MK-2206 suppresses Akt signalling pathway and promoting cancer cell death as a single agent as well as in combination with other chemotherapeutic agents. MK-2206 enhance the sensitivity to through apoptosis and enhance the sensitivity to rapamycin via reactive oxygen species. Combination of MK-2206 with etoposide or rapamycin significantly increase antitumor growth effect.
References
1. Pant A, Lee II, Lu Z, Rueda BR, Schink J, Kim JJ.Inhibition of AKT with the Orally Active Allosteric AKT Inhibitor, MK-2206, Sensitizes Endometrial Cancer Cells to Progestin.PLoS One. 2012;7(7):e41593. Epub 2012 Jul 24.
2. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. TA Yap, L Yan, A Patnaik, I Fearen. Journal of Clinical Oncology 2011

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