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mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells
In Vitro
mTOR inhibitor-8 (Compound 5e; 0.1-10 μM; 24 and 48 hours) suppresses the growth of A549 cells in a dose-dependent manner. mTOR inhibitor-8 induces autophagy in an mTOR-dependent manner. mTOR inhibitor-8 (10 μM; 3-24 hours) induces autophagy in a time-dependent manner. The levels of LC3B-II are enhanced. mTOR inhibitor-8 (10 μM; 3-24 hours) reduces the phosphorylation of RPS6KB1 (ribosomal protein S6 kinase) and EIF4EBP1 (eukaryotic translation initiation factor 4E-binding protein 1), two essential substrates of mTORMCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549 cells Concentration: 0.1, 1, 5, 10 μM Incubation Time: 24 and 48 hours Result: Suppressed the growth of A549 cells with an IC 50 of 2.6±0.11 μM. Western Blot AnalysisCell Line: A549 cells Concentration: 10 μM Incubation Time: 3, 6, 12 and 24 hours Result: The levels of phosphorylation of RPS6KB1 and EIF4EBP1 were significantly decreased after treatment.
In Vivo
mTOR inhibitor-8 (25 and 50 μM; 6 days) effectively inhibits tumor growth in vivo without adverse effect on normal chick chorioallantoic membrane angiogenesis . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Fertile chicken eggs (7-9 days old) Dosage: 25 and 50 μM Administration: 6 days Result: Significant xenograft tumor remission was observed in eggs compared with the DMSO-treated eggs.
IC50& Target:mTOR Autophagy
| Molecular Weight | 446.95 |
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