Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(MK-2206 dihydrochloride; MK-2206; MK2206)
MK 2206 Chemical Structure
|Product name: MK 2206|
|Cat. No.: HY-10358|
MK-2206 2Hcl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed.
IC50 value: 8 nM/12 nM/65 nM(Akt1/2/3) 
in vitro: MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins . MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells . MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death .
in vivo: MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg . MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib .
|M.Wt||480.39||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥92mg/mL Water ≥92mg/mL Ethanol ≥1.8mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.0816 mL||10.4082 mL||20.8164 mL|
|5 mM||0.4163 mL||2.0816 mL||4.1633 mL|
|10 mM||0.2082 mL||1.0408 mL||2.0816 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|MK 2206||National Cancer Institute||Gallbladder tumor||31-JAN-13||31-MAY-13||Phase 2||11-OCT-13|
|National Cancer Institute||Biliary cancer||31-JAN-13||31-MAY-13||Phase 2||11-OCT-13|
|National Cancer Institute||Breast tumor||31-JAN-13||31-MAR-16||Phase 2||25-SEP-13|
|National Cancer Institute||Metastatic pancreas cancer||31-AUG-12||Phase 2||17-JUL-13|
|Washington University in St Louis||Breast tumor||30-JUN-13||31-AUG-15||Phase 2||21-JUN-13|
|National Cancer Institute||Metastatic colorectal cancer||31-MAR-13||01-SEP-14||Phase 2||12-SEP-13|
. Hirai H, 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 Therapy, 2010, 9(7), 1956-1967.
. Cheng Y, et al. eEF-2 kinase dictates cross-talk between autophagy and apoptosis induced by Akt Inhibition, thereby modulating cytotoxicity of novel Akt inhibitor MK-2206. Cancer Res, 2011, 71(7), 2654-2663.
3CAI is a potent allosteric and specific AKT inhibitor, which exerts efficacy in vitro and in vivo.
A-443654 is a potent small-molecule inhibitor of all three Akt serine/threonine kinases, induces Akt Ser-473 phosphorylation in all human cancer cell lines tested, including PTEN- and TSC2-deficient lines.
AKT inhibitor is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKB(alpha) (IC50 = 0.5 nM) than PKA (IC50=450 nM).
Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.
AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity; AKT, p70S6K, PKA, ROCK, and SGK inhibitor.
AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).
CCT128930 is a novel potent ATP-competitive, selective Akt2 inhibitor with an IC50 of 6 nM; >28-fold selectivity for Akt2 than the closely related PKA kinase.
Deguelin, a naturally occurring rotenoid, is known to be an Akt inhibitor and to have an anti-tumor effect on several cancers; decrease levels of phosphorylated Akt.
LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).
Perifosine (KRX-0401; D-21266; NSC 639966) is a novel Akt inhibitor with IC50 of 4.7 (mu)M, targets pleckstrin homology domain of Akt.