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HY-10358

CAS:1032350-13-2

 (Synonyms  MK-2206 dihydrochloride;MK2206 dihydrochloride)
1032350-13-2  Technical Data: Price and Availability of  Cas No:1032350-13-2

Cas : 1032350-13-2 M.Wt: 480.39
Cas : 1032350-13-2 Formula: C25H23Cl2N5O
Cas : 1032350-13-2 Purity: >98 %
Cas : 1032350-13-2 Storage: at 20℃ 2 years
Cas : 1032350-13-2 Solubility: DMSO ≥92mg/mL Water ≥92mg/mL Ethanol ≥1.8mg/mL
Cas : 1032350-13-2 Name: MK 2206 (dihydrochloride)
USD
5mg/$80 In-stock
10mg/$110 In-stock
50mg/$260 In-stock
100mg/$400 In-stock
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1032350-13-2  Data Sheet:
 
Introduction of 1032350-13-2 :
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].
 
References on 1032350-13-2 :
 

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