Flupentixol
Based on 2 publication(s) in Google Scholar
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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- CAS. Nr.: 2709-56-0
- Formel: C23H25F3N2OS
- Molecular Weight:434.52
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Flupentixol
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Biologische Aktivität
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D1 Receptor |
D2 Receptor |
PI3Kα 127 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Astrocyte | EC50 |
1.182 μM
Compound: 7
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
| HEK293 | IC50 |
89.5 μM
Compound: flupenthixol
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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
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[PMID: 18788725] |
| Medulloblastoma cell | EC50 |
0.187 μM
Compound: 7
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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
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[PMID: 17417631] |
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.
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Cell Line:A549, H661, SK-SEM-1, and NCAL-H520 cells
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Concentration:2.5, 5, 10, 20, or 40 μM
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Incubation Time:72 hours
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Result:Showed the IC50s of 5.708 μM and 6.374 μM for A549 and H661 cells, respectively.
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Cell Line:A549 and H661 cells
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Concentration:5, 10, 20 and 40 μM
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Incubation Time:24 hours
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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.
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Cell Line:H661 and A549 cells
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Concentration:2.5, 5, 10, and 15 μM
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Incubation Time:24 hours
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Result:Decreased AKT phosphorylation levels in a dose-dependent manner, decreased the expression levels of Bcl-2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude mice injected with A549 cells[3]
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Dosage:40 mg/kg
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Administration:Intragastric injection; 40 mg/kg; once daily; 21 days
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Result:Reduced tumor volumes compared to the vehicle control (p<0.05), reduced tumor weights by 64.1% (p<0.05).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2709-56-0
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Molecular Weight 434.52
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Formel C23H25F3N2OS
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SMILES
OCCN1CCN(CC/C=C2C3=C(SC4=C/2C=CC=C4)C=CC(C(F)(F)F)=C3)CC1
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Synonyms
Flupenthixol
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998
Reinheit & Dokumentation
Verweise
[1]. Yonar D, et al. Effect of cis-(Z)-flupentixol on DPPC membranes in the presence and absence of cholesterol. Chem Phys Lipids. 2016 Jun;198:61-71. [Content Brief]
[2]. Ruhrmann S, et al. Efficacy of flupentixol and risperidone in chronic schizophrenia with predominantly negative symptoms. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Jun 30;31(5):1012-22. [Content Brief]
[3]. Chao Dong, et al. The antipsychotic agent flupentixol is a new PI3K inhibitor and potential anticancer drug for lung cancer. Int J Biol Sci. 2019 Jun 2;15(7):1523-1532. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Flupentixol Related Classifications
HY-15856A Related Classifications
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