1. PI3K/Akt/mTOR
    Autophagy
  2. mTOR
    Autophagy
  3. mTOR inhibitor-8

mTOR inhibitor-8 

Cat. No.: HY-131344
Handling Instructions

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.

For research use only. We do not sell to patients.

mTOR inhibitor-8 Chemical Structure

mTOR inhibitor-8 Chemical Structure

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Description

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[1].

IC50 & Target[1]

mTOR

 

Autophagy

 

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[1].
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[1].
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 mTOR[1]

Cell Viability Assay[1]

Cell 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 IC50 of 2.6±0.11 μM.

Western Blot Analysis[1]

Cell 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[1].

Animal Model: Fertile chicken eggs (7-9 days old)[1]
Dosage: 25 and 50 μM
Administration: 6 days
Result: Significant xenograft tumor remission was observed in eggs compared with the DMSO-treated eggs.
Molecular Weight

446.95

Formula

C₂₄H₁₉ClN₄OS

SMILES

COC1=CC=C(C2CC(C3=CC=C(Cl)C=C3)=NN2C4=NC(C5=CC=NC=C5)=CS4)C=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

mTOR inhibitor-8mTOR inhibitor8mTOR inhibitor 8mTORAutophagyMammalian target of RapamycinautophagyinducerFKBP12A549humanlungcancercellsInhibitorinhibitorinhibit

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mTOR inhibitor-8
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HY-131344
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