2. PI3K/Akt/mTOR Apoptosis
  3. PI3K mTOR Apoptosis Bcl-2 Family MDM-2/p53 Caspase
  4. 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).

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

PI3K/mTOR-IN-17 Chemical Structure

PI3K/mTOR-IN-17 Chemical Structure

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PI3K/mTOR-IN-17 Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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mTOR mTORC1 mTORC2

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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)[1].

IC50 & Target

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.

PI3K/mTOR-IN-17 Related Antibodies

Real Time qPCR[1]

Cell Line: A549 lung cancer cells
Concentration: 1.39 μM
Incubation Time: 48 h
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.

Apoptosis Analysis[1]

Cell Line: A549 lung cancer cells
Concentration: 1.39 μM
Incubation Time: 48 h
Result: Significantly induced, increasing 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.

ELISA Assay[1]

Cell Line: A549 lung cancer cells
Concentration: 1.39 μM
Incubation Time: 48 h
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.
Molecular Weight

618.68

Formula

C36H34N4O6
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PI3K/mTOR-IN-17 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI3K/mTOR-IN-17PI3KmTORApoptosisBcl-2 FamilyMDM-2/p53CaspasePhosphoinositide 3-kinaseMammalian target of RapamycinCaspasesBax/Bcl-2P53Non-small cell lung cancer (NSCLC)A549 cellslung fibroblasts WI-38Inhibitorinhibitorinhibit

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