MK-2206 (dihydrochloride) [1032350-13-2]

Catalog number: HY-10358_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: 5 mg
10 mM
10 mg
50 mg
200 mg
Price: € 308.00
Expected delivery time: 10 days
Quantity:

Product specifications for - MK-2206 (dihydrochloride) [1032350-13-2]

Overview: 
Product group: Chemicals
Category: Other
CAS No.: 1032350-13-2
Properties: 
Purity: >98%
Molecular Formula: C25H23Cl2N5O
Molecular weight: 480.39
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: 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].
Safety information: 
MSDS: MSDS
Establishment and characterization of six novel hepatocellular carcinoma cell lines from Chinese patient-derived tumor xenografts', Xin-Yun Zhang. Int J Clin Exp Pathol. 2017;10(3):3033-3042. Read more
Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma', Kiessling MK. PLoS One. 2016 Jan 28;11(1):e0147682. Read more
Inhibition of phosphorylated Ser473-Akt from translocating into the nucleus contributes to 2-cell arrest and defective zygotic genome activation in mouse preimplantation embryogenesis', Junming Chen. Dev Growth Differ. 2016 Apr;58(3):280-92. Read more
Abl kinase regulation by BRAF/ERK and cooperation with Akt in melanoma', Jain A. Oncogene. 2017 Aug 10;36(32):4585-4596. Read more
αMSH inhibits adipose inflammation via reducing FoxOs transcription and blocking Akt/JNK pathway in mice', Liu G. Oncotarget. 2017 Jul 18;8(29):47642-47654. Read more
STYK1 promotes cancer cell proliferation and malignant transformation by activating PI3K-AKT pathway in gallbladder carcinoma', Hu YP. Int J Biochem Cell Biol. 2018 Jan 31;97:16-27. Read more