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100mg | ||
250mg | ||
500mg |
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 |
Intranastric injections of flupentixol (40 mg/kg, once daily for 21 days) prevent the formation of A549 xenograft tumors in mice that are not clothed [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: H661 and A549 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 |
C23H25N2OF3S
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Molecular Weight |
434.5176
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CAS # |
2709-56-0
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Related CAS # |
Flupentixol dihydrochloride;2413-38-9;cis-(Z)-Flupentixol dihydrochloride;51529-01-2
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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=C2\C3=CC=CC=C3SC3C=CC(=CC\2=3)C(F)(F)F)CC1
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3014 mL | 11.5070 mL | 23.0139 mL | |
5 mM | 0.4603 mL | 2.3014 mL | 4.6028 mL | |
10 mM | 0.2301 mL | 1.1507 mL | 2.3014 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.