2. PI3K/Akt/mTOR Apoptosis Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. PI3K mTOR Apoptosis Bcl-2 Family MDM-2/p53 Telomerase Mitochondrial Metabolism
  4. 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.

PI3K/mTOR-IN-19

PI3K/mTOR-IN-19 Chemical Structure

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PI3K/mTOR-IN-19 Related Antibodies

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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 BNIP3

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Description

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[1].

IC50 & Target

PI3K

4.23 nM (IC50)

mTOR

2.3 nM (IC50)

Bax

 

Bcl-2

 

In Vitro

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.

PI3K/mTOR-IN-19 Related Antibodies

Cell Proliferation Assay[1].

Cell Line: HeLa cells, MCF-7 cells, HepG-2 cells, A549 cells, Eca109 cells, MCF12A cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 48 h
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)

Cell Proliferation Assay[1].

Cell Line: TE1, TE13, KYSE30, KYSE70, KYSE150
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
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)

Apoptosis Analysis[1].

Cell Line: Eca109 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Significantly increased proportion of Annexin V/PI positive cells indicates an increase in early and late apoptotic cells.
In Vivo

PI3K/mTOR-IN-19 (Compound 8e) (2-5 mg/kg, i.p., 3 times a week for 14 days) exhibits dose-dependent tumor growth inhibition in Eca109 cell xenograft mice, with no significant toxicity observed[1].

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

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].
Dosage: 2 mg/kg, 5 mg/kg, 10 mg/kg
Administration: I.p., 3 times a week for 14 days
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.
Molecular Weight

465.52

Formula

C25H28FN5O3
SMILES

O=C(OCCN(CC)CC)C1=CC=C(N2N=NC(C3=NOC(C4=CC=C(F)C=C4)=C3)C2C)C=C1
Shipping

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-19 Related Classifications

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  • 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-19PI3KmTORApoptosisBcl-2 FamilyMDM-2/p53TelomeraseMitochondrial MetabolismPhosphoinositide 3-kinaseMammalian target of Rapamycincell cycleoxidative stresscytokinespharmacokineticsInhibitorinhibitorinhibit

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