PI3K/mTOR-IN-19
PI3K/mTOR-IN-19 is an orally active, potent, selective PI3K (IC50 = 4.23 nM) and mTOR (IC50 = 2.3 nM) inhibitor. PI3K/mTOR-IN-19 significantly inhibits Eca109 cell viability and induces apoptosis. PI3K/mTOR-IN-19 causes G0/G1 cell cycle arrest, decreased mitochondrial membrane potential, and demonstrates marked telomerase inhibitory activity. PI3K/mTOR-IN-19 modulates the expression of key apoptotic regulators (Bcl-2, Bax, and p53) and downregulates the PI3K/Akt/mTOR signaling pathway. PI3K/mTOR-IN-19 can be used for the study of esophageal cancer.
For research use only. We do not sell to patients.
- Formula: C25H28FN5O3
- Molecular Weight:465.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3K 4.23 nM (IC50) |
mTOR 2.3 nM (IC50) |
Bax |
Bcl-2 |
PI3K/mTOR-IN-19 (Compound 8e) (2.5-10 μM, 48-72 h) exhibits the most significant inhibitory activity against a variety of cancer cell lines, particularly demonstrating substantial inhibition of numerous ESCC cell lines, shows minimal cytotoxicity in non-tumorigenic epithelial cells, and dose-dependently inhibits Eca109 cell proliferation while inducing cytotoxic morphological changes[1].
PI3K/mTOR-IN-19 (2.5-10 μM, 24 h) induces apoptosis, inhibits migration and invasion potential, and increases the proportion of cells in G0/G1 phase while decreasing the proportion in S and G2 phases in Eca109 cells[1].
PI3K/mTOR-IN-19 inhibits telomerase activity by 71.5% in Eca109 cells[1].
PI3K/mTOR-IN-19 (2.5-10 μM, 24 h) reduces the mitochondrial membrane potential (ΔΨm), which is manifested as a decrease in the red/green fluorescence ratio in Eca109 cells[1].
PI3K/mTOR-IN-19 (2.5-10 μM) upregulates p53 and Bax expression and downregulates Bcl-2 expression; it also reduces p-PI3K, p-Akt (Ser473), and p-mTOR levels in Eca109 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells, MCF-7 cells, HepG-2 cells, A549 cells, Eca109 cells, MCF12A cells
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:48 h
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Result:Cervical cancer (HeLa, IC50 = 23.12 µM)
Human breast cancer cell line (MCF-7, IC50 = 22.03 µM)
Liver cancer cell line (HepG-2, IC50 = 16.72 µM)
Lung cancer cell line (A549, IC50 = 17.78 µM)
Esophageal cancer (Eca109, IC50 = 0.28 µM)
Non-tumorigenic epithelial cell (MCF12A, IC50 ＞ 250 µM)
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Cell Line:TE1, TE13, KYSE30, KYSE70, KYSE150
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:TE1 (IC50 = 1.34 μM) TE13 (IC50 = 2.78 μM) KYSE30 (IC50 = 1.23 μM) KYSE70 (IC50 = 1.11 μM) KYSE150 (IC50 = 1.05 μM)
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Cell Line:Eca109 cells
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Significantly increased proportion of Annexin V/PI positive cells indicates an increase in early and late apoptotic cells.
| Species | Dose | Route | T1/2 | Cmax | Tmax | AUC | F |
|---|---|---|---|---|---|---|---|
| Rat | 10 mg/kg | i.v. | 3.42 h | 1.27 μg/mL | 0 h | 6270 ng·h/mL | / |
| Rat | 10 mg/kg | p.o. | 9.22 h | 2.11 μg/mL | 2 h | 28060 ng·h/mL | 89.5 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A subcutaneous injection of 1×106 Eca109 cells with Matrigel at a dilution of 1:1 was administered to the right flank region of every single male BALB/c null nude mice (6-week-old)[1].
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Dosage:2 mg/kg, 5 mg/kg, 10 mg/kg
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Administration:I.p., 3 times a week for 14 days
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Result:MDA levels were decreased, while SOD and GSH activities were increased.
The expression of TNF-α, IL-1β, and IL-6 was significantly inhibited.
The expression of PI3K and p-Akt (Ser473) proteins in tumor tissues was significantly reduced.
Chemical Information
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Molecular Weight 465.52
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Formula C25H28FN5O3
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SMILES
O=C(OCCN(CC)CC)C1=CC=C(N2N=NC(C3=NOC(C4=CC=C(F)C=C4)=C3)C2C)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3K/mTOR-IN-19 Related Classifications
HY-179155 Related Classifications
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