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GSK2126458 Chemical Structure
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Biological Activity
GSK2126458 is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic and tumor growth efficacy models. In cell, in good agreement with the inhibition of potent PI3K. GSK2126458 reduced the phosphorylated AKT, p70S6K contents in a dose and time dependent way, as well as the prevention of PRAS40 and ERK. The IC50 of GSK2126458 is 2 nM for pAKT in the HCC1954 breast carcinoma cell line. In various human tumor cells, GSK2126458 had a width of inhibitory activity for potent cell growth and induced cell death. Notably, GSK2126458 acted mainly by not induction of apoptosis but cell cycle arrest, particularly in G1-phase. [1][2]
Chemical Information
| Molecular Weight (WM): | 505.5 |
|---|---|
| Formula: | C25H17F2N5O3S |
| CAS No.: | 1086062-66-9 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥101mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of GSK2126458 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of GSK2126458 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
Data independently produced by Dr. Zhang of Tianjin Medical University GSK2126458 purchased from Selleck
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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of GSK2126458 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
Data independently produced by Dr. Zhang of Tianjin Medical University
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