1. PI3K/Akt/mTOR Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  2. Akt Apoptosis mTOR PI3K Microtubule/Tubulin
  3. PI3K/Akt/mTOR-IN-4

PI3K/Akt/mTOR-IN-4 (compound 4r) is a potent PI3K/Akt/mTOR and tubulin polymerization inhibitor. PI3K/Akt/mTOR-IN-4 induce apoptosis and cell cycle arrest at G2/M phase. PI3K/Akt/mTOR-IN-4 decreases the expression of p-PI3K, p-Akt, and p-mTOR, β-tubulin.

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PI3K/Akt/mTOR-IN-4

PI3K/Akt/mTOR-IN-4 Chemical Structure

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Description

PI3K/Akt/mTOR-IN-4 (compound 4r) is a potent PI3K/Akt/mTOR and tubulin polymerization inhibitor. PI3K/Akt/mTOR-IN-4 induce apoptosis and cell cycle arrest at G2/M phase. PI3K/Akt/mTOR-IN-4 decreases the expression of p-PI3K, p-Akt, and p-mTOR, β-tubulin[1].

Cellular Effect
Cell Line Type Value Description References
Ca-Ski IC50
7.24 μM
Compound: 4r
Antiproliferative activity against human Ca-Ski cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human Ca-Ski cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
HEK-293T IC50
23.96 μM
Compound: 4r
Cytotoxicity against human HEK293T cells assessed as cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HEK293T cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
HeLa IC50
5.03 μM
Compound: 4r
Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
L02 IC50
21.08 μM
Compound: 4r
Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
SiHa IC50
3.38 μM
Compound: 4r
Antiproliferative activity against human SiHa cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SiHa cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
In Vitro

PI3K/Akt/mTOR-IN-4 (compound 4r) (0-100 µM; 48 h) shows antiproliferative activity with IC50s of 3.38, 5.03, 7.24, 21.08, 23.96 µM for SiHa, HeLa, Ca Ski, LO2, HEK-293t cells, respectively[1].
PI3K/Akt/mTOR-IN-4 (0-16 µM; 24 h) induces apoptosis and cell cycle arrest at G2/M phase[1].
PI3K/Akt/mTOR-IN-4 (4, 8,16 µM; 24 h) decreases the expression of phosphorylation of PI3K, Akt, mTOR level and β-tubulin protein in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: SiHa, HeLa, Ca Ski, LO2, HEK-293t cells
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Inhibited cell proliferative with IC50s of 3.38, 5.03, 7.24, 21.08, 23.96 µM for SiHa, HeLa, Ca Ski, LO2, HEK-293t cells, respectively.

Cell Cycle Analysis[1]

Cell Line: SiHa cells
Concentration: 0-16 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G2/M phase with G2/M phase cells accumulating from 5.24 % (Ctrl) to 28.37 % (16 μM).

Apoptosis Analysis[1]

Cell Line: SiHa cells
Concentration: 0-16 µM
Incubation Time: 24 h
Result: Induced apoptosis the percentage of apoptotic cells were increased from 11.62 % (Ctrl) to 98.56 % (16 μM).

Western Blot Analysis[1]

Cell Line: SiHa cells
Concentration: 4, 8, 16 μM
Incubation Time: 24 h
Result: Decreased the expression of phosphorylation of PI3K, Akt, and mTOR, β-tubulin in a dose-dependent manner.
In Vivo

PI3K/Akt/mTOR-IN-4 (0-400 μM; 0-96 h) shows no toxicity for zebrafish embryos[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: zebrafish embryos[1]
Dosage: 0, 12.5, 25, 50, 100, 200, 400 μM
Administration: 0-96 h
Result: Showed no toxicity for zebrafish embryos.
Molecular Weight

500.56

Formula

C29H29FN4O3

SMILES

COC1=C(OC)C(OC)=CC(C2=NC3=CC(N4CCN(C)CC4)=C(C#CC5=CC=CC=C5F)C=C3N2)=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.

Purity & Documentation
References
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Product Name:
PI3K/Akt/mTOR-IN-4
Cat. No.:
HY-163511
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