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Products are for research use only. Not for human use. We do not sell to patients.

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MK 2206

HY-10358

(MK-2206 dihydrochloride; MK-2206; MK2206)

MK 2206

MK 2206 Chemical Structure

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.

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10 mM * 1 mL in DMSO $121 In-stock
10 mg $110 In-stock
50 mg $260 In-stock
100 mg $400 In-stock
200 mg Get quote
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Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €119 In-stock
10 mg €108 In-stock
50 mg €255 In-stock
100 mg €392 In-stock
200 mg Get quote
500 mg Get quote

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Product name: MK 2206
Cat. No.: HY-10358

MK 2206 Data Sheet

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    Purity: 98.58%

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Biological Activity of MK 2206

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) [1]
Target: 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 [1]. 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 [2]. 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 [3].
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 [1]. MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib [2].
 

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 480.39 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H23Cl2N5O
CAS No 1032350-13-2
Solvent & Solubility

DMSO ≥92mg/mL Water ≥92mg/mL Ethanol ≥1.8mg/mL

Preparing Stock Solutions

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

Clinical Information of MK 2206

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

References on MK 2206

Inhibitor Kit

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