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MK 2206 dihydrochloride CAS: 1032350-13-2

Category: Inhibitors
Product Name: MK 2206 dihydrochloride
Cat No: I000192
CAS No: 1032350-13-2
Synonyms: 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride
Molecular Formula: C25H21N5O • 2HCl
Molecular Weight: 480.4
SMILES: NC1(CCC1)C(C=C2)=CC=C2C(C(C3=CC=CC=C3)=C4)=NC5=C4C(N6C=C5)=NNC6=O.Cl.Cl
Solubility: DMSO ≥92mg/mL Water ≥92mg/mL Ethanol ≥1.8mg/mL
Target: Akt
IC50: 8 nM/12 nM/65 nM(Akt1/2/3) [1]
Storage: powder
CAS 1032350-13-2,MK 2206 dihydrochloride
  • Description

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].

  • Spec

Appearance:A crystalline solid

  • References

[1]. Yan L, AACR Annual Meeting 2009: Abstract Number: DDT01-1.
[2]. 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.
[3]. 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.

price inquiry for CAS:1032350-13-2, Product:MK 2206 dihydrochloride