China (Mainland)
MK-2206 2HCl CAS NO.1032350-13-2
- Min.Order: 5 Metric Ton
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- Product Details
Keywords
- MK-2206 2HCl
- 1032350-13-2
- Akt inhibitor
Quick Details
- ProName: MK-2206 2HCl
- CasNo: 1032350-13-2
- Molecular Formula: C25H21N5O.2HCl
- ProductionCapacity: Metric Ton/Day
- Purity: >97%
- LimitNum: 5 Metric Ton
Superiority
Biological Activity
| Description | MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2. | ||||||||||||||||||||||||||||||
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| Features | The first allosteric small molecule inhibitor of Akt to enter clinical development. | ||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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] |