2. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR Apoptosis
  3. Dopamine Receptor PI3K Apoptosis
  4. 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 Estructura química

No. CAS : 2709-56-0

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Flupentixol Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Descripciòn

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)

Cellular Effect
Cell Line Type Value Description References
Astrocyte EC50
1.182 3
Compound: 7
Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
[PMID: 17417631]
HEK293 IC50
89.5 3
Compound: Flupentixole
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HEK293 IC50
89.5 3
Compound: flupenthixol
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
Medulloblastoma cell EC50
0.187 3
Compound: 7
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
[PMID: 17417631]
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.

Flupentixol Related Antibodies

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).
Ensayo clínico
Peso molecular

434.52

Fòrmula

C23H25F3N2OS
No. CAS
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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Flupentixol Related Classifications

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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.

Keywords:

Flupentixol2709-56-0FlupenthixolDopamine ReceptorPI3KApoptosisPhosphoinositide 3-kinaseanti-proliferative activityinduce apoptosisschizophreniaanxiolyticdepressiveA549H661SK-SEM-1NCAL-H520Inhibitorinhibitorinhibit

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