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

Flupentixol  (Synonyms: Flupenthixol)

Cat. No.: HY-15856A
Handling Instructions

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.

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

Flupentixol Chemical Structure

Flupentixol Chemical Structure

CAS No. : 2709-56-0

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Description

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).
Clinical Trial
Molecular Weight

434.52

Formula

C23H25F3N2OS

CAS No.
SMILES

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

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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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.

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Flupentixol
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HY-15856A
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