1. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR Apoptosis
  2. Dopamine Receptor PI3K Apoptosis
  3. Flupentixol

Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.

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Flupentixol

Flupentixol Chemische Struktur

CAS. Nr. : 2709-56-0

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Beschreibung

Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research[1][2][3].

IC50 & Target[3]

D1 Receptor

 

D2 Receptor

 

PI3Kα

127 nM (IC50)

In Vitro

Flupentixol (2.5-40 μM; 72 h) treatment inhibits the viability of lung cancer cells in a dose-dependent manner[3].
Flupentixol (2.5-40 μM; 24 h) induces apoptosis in lung cancer cells[3].
Flupentixol (2.5-15 μM; 24 h) inhibits p-AKT and Bcl-2 expression levels[3].

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

Cell Viability Assay[3]

Cell Line: A549, H661, SK-SEM-1, and NCAL-H520 cells
Concentration: 2.5, 5, 10, 20, or 40 μM
Incubation Time: 72 hours
Result: Showed the IC50s of 5.708 μM and 6.374 μM for A549 and H661 cells, respectively.

Apoptosis Analysis[3]

Cell Line: A549 and H661 cells
Concentration: 5, 10, 20 and 40 μM
Incubation Time: 24 hours
Result: Increased the percentage of cells in early apoptosis compared with the negative control in both A549 and H661 (p< 0.05). Induced the cleavage of PARP and caspase-3 in a dose-dependent manner.

Western Blot Analysis[3]

Cell Line: H661 and A549 cells
Concentration: 2.5, 5, 10, and 15 μM
Incubation Time: 24 hours
Result: Decreased AKT phosphorylation levels in a dose-dependent manner, decreased the expression levels of Bcl-2.
In Vivo

Flupentixol (intragastric injection; 40 mg/kg; once daily; 21 d) suppresses A549 xenografted tumor growth in nude mice[3].

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

Animal Model: BALB/C nude mice injected with A549 cells[3]
Dosage: 40 mg/kg
Administration: Intragastric injection; 40 mg/kg; once daily; 21 days
Result: Reduced tumor volumes compared to the vehicle control (p<0.05), reduced tumor weights by 64.1% (p<0.05).
Klinische Studie
Molekulargewicht

434.52

Formel

C23H25F3N2OS

CAS. Nr.
SMILES

OCCN1CCN(CC/C=C2C3=C(SC4=C/2C=CC=C4)C=CC(C(F)(F)F)=C3)CC1

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

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