| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Treatment with flupentixol (2.5-40 μM; 72 h) dose-dependently reduces lung cancer cell viability [3]. To induce apoptosis in lung cancer cells, administer flupentixol (2.5-40 μM) for 24 hours [3]. Bcl-2 expression levels and p-AKT are inhibited by flupentixol (2.5–15 μM; 24 hours) [3].
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| ln Vivo |
Flupentixol (intragastric injection; 40 mg/kg; once daily; 21 days) suppresses the formation of A549 xenograft tumors in nude mice [3].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: A549, H661, SK-SEM-1 and NCAL-H520 Cell Tested Concentrations: 2.5, 5, 10, 20 or 40 μM Incubation Duration: 72 hrs (hours) Experimental Results: Shows IC50 of 5.708 μM A549 and H661 Cells were 6.374 μM and 6.374 μM respectively. Apoptosis analysis[3] Cell Types: A549 and H661 Cell Tested Concentrations: 5, 10, 20 and 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: The percentage of early apoptotic cells increased in A549 and H661 compared to the negative control (p < 0.05). Induces PARP and caspase-3 cleavage in a dose-dependent manner. Western Blot Analysis [3] Cell Types: A549 and H661 Cell Tested Concentrations: 2.5, 5, 10 and 15 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished AKT phosphorylation levels and diminished Bcl-2 expression levels in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: BALB/C nude mice injected with A549 cells [3]
Doses: 40 mg/kg Route of Administration: gavage; 40 mg/kg; one time/day; 21 days Experimental Results: Compared with the vehicle control, the tumor volume diminished ( p<0.05), tumor weight diminished by 64.1% (p<0.05). |
| References |
[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.
[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. [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. |
| Molecular Formula |
C23H25F3N2OS.2(HCL)
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|---|---|
| Molecular Weight |
507.44
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| CAS # |
2413-38-9
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| Related CAS # |
cis-(Z)-Flupentixol dihydrochloride;51529-01-2;Flupentixol;2709-56-0
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~197.07 mM)
DMSO : ~33.33 mg/mL (~65.68 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (98.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9707 mL | 9.8534 mL | 19.7068 mL | |
| 5 mM | 0.3941 mL | 1.9707 mL | 3.9414 mL | |
| 10 mM | 0.1971 mL | 0.9853 mL | 1.9707 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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