PI3K/mTOR-IN-17
PI3K/mTOR-IN-17 is a dual PI3K and mTOR inhibitor with IC50 values of 1.21 μM (PI3K), and 0.21 μM (mTOR). PI3K/mTOR-IN-17 induces cells caspase-mediated apoptosis by arresting their growth in the G1-phase. PI3K/mTOR-IN-17 upregulates the levels of caspases-3, 7, 8, and 9, p53 expression and Bax/Bcl-2 ratio. PI3K/mTOR-IN-17 suppresses the PI3K/mTOR signaling pathway. PI3K/mTOR-IN-17 can be used for research of cancer, such as non-small cell lung cancer (NSCLC).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C36H34N4O6
- Molecular Weight:618.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PI3K 1.21 μM (IC50) |
mTOR 0.21 μM (IC50) |
Caspase 3 |
Caspase-7 |
Caspase-8 |
Caspase-9 |
Bax |
Bcl-2 |
In Vitro
PI3K/mTOR-IN-17 (Compound 8) shows superior cytotoxicity with IC50 values of 21.13 μM (lung fibroblasts WI-38) and 1.39 μM (A549 cells), and selectivity index of 15.32[1].
PI3K/mTOR-IN-17 (1.39 μM, 48 h) upregulates the leves of p53 and Bax, and downregulates the leves of Bcl-2, EGFR, PI3K and mTOR in A549 cells[1].
PI3K/mTOR-IN-17 (1.39 μM, 48 h) upregulates the initiator caspase-8 and 9 levels and the executioner caspases-3 and 7 levels in A549 cells[1].
PI3K/mTOR-IN-17 (1.39 μM, 48 h) induces significantly apoptosis by arresting their growth in the G1-phase in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 lung cancer cells
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Concentration:1.39 μM
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Incubation Time:48 h
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Result:Significantly increased the expression of p53 by 8.38 folds Bax by 9.88 fold and downregulated the leves of Bcl-2 by 0.45 fold.
Suppressed gene expression of EGFR by 0.42 fold, PI3K by 0.45 fold, and mTOR by 0.58 fold.
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Cell Line:A549 lung cancer cells
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Concentration:1.39 μM
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Incubation Time:48 h
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Result:Significantly increased the overall death rate by 21 fold.
Total apoptosis reached 25.03% (19.38% late apoptosis, 5.65% early apoptosis) compared to 1.19% in the untreated control group.
Markedly increased the cell population in the G1-phase to 80.2% compared to 57.3% in the control, and reduced the proportions of cells in the S and G2/M phases.
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Cell Line:A549 lung cancer cells
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Concentration:1.39 μM
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Incubation Time:48 h
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Result:Upregulated the initiator caspase-8 and 9 levels by almost 2.2 and 1.03 fold and the executioner caspases-3 and 7 by 1.73 and 1.34 fold.
Chemical Information
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Molecular Weight 618.68
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Formel C36H34N4O6
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SMILES
O=C(N1C2=CC=C(NC(C(C3=CC=CC=C3)N(C4=CC=C(C)C=C4)C(CNC(OC(C)(C)C)=O)=O)=O)C=C2)C5=CC=CC=C5C1=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PI3K/mTOR-IN-17 Related Classifications
HY-174855 Related Classifications
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