Flupentixol dihydrochloride
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.52%
- CAS. Nr.: 2413-38-9
- Formel: C23H27Cl2F3N2OS
- Molecular Weight:507.44
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Flupentixol dihydrochloride
MoreAlle Dopamine Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
PI3Kα 127 nM (IC50) |
D1 Receptor |
D2 Receptor |
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. Further protocols information, click here.
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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:A549 and H661 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.
In Vivo
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).
Chemical Information
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CAS. Nr. 2413-38-9
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Appearance Solid
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Molecular Weight 507.44
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Formel C23H27Cl2F3N2OS
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Color White to off-white
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SMILES
OCCN1CCN(CC/C=C2C3=C(SC4=C/2C=CC=C4)C=CC(C(F)(F)F)=C3)CC1.[H]Cl.[H]Cl
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Synonyms
Flupenthixol dihydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
Lösungsmittel & Löslichkeit
In Vitro:
H2O : 100 mg/mL (197.07 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (65.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (98.53 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 1.9707 mL | 9.8534 mL | 19.7068 mL | 49.2669 mL |
| 5 mM | 0.3941 mL | 1.9707 mL | 3.9414 mL | 9.8534 mL | |
| 10 mM | 0.1971 mL | 0.9853 mL | 1.9707 mL | 4.9267 mL | |
| 15 mM | 0.1314 mL | 0.6569 mL | 1.3138 mL | 3.2845 mL | |
| 20 mM | 0.0985 mL | 0.4927 mL | 0.9853 mL | 2.4633 mL | |
| 25 mM | 0.0788 mL | 0.3941 mL | 0.7883 mL | 1.9707 mL | |
| 30 mM | 0.0657 mL | 0.3284 mL | 0.6569 mL | 1.6422 mL | |
| 40 mM | 0.0493 mL | 0.2463 mL | 0.4927 mL | 1.2317 mL | |
| 50 mM | 0.0394 mL | 0.1971 mL | 0.3941 mL | 0.9853 mL | |
| 60 mM | 0.0328 mL | 0.1642 mL | 0.3284 mL | 0.8211 mL | |
| H2O | 80 mM | 0.0246 mL | 0.1232 mL | 0.2463 mL | 0.6158 mL |
| 100 mM | 0.0197 mL | 0.0985 mL | 0.1971 mL | 0.4927 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Flupentixol dihydrochloride Related Classifications
HY-15856B Related Classifications
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