Size | Price | |
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50mg | ||
100mg | ||
250mg |
ln Vitro |
The growth of esophageal squamous cell carcinoma (ESCC) cells is inhibited by propafenone (5–25 μM) [3]. Propafenone reduces the potential of the mitochondrial membrane and decreases the expression of Bcl-xL and Bcl-2, which results in mitochondrial malfunction [3]. The anti-apoptotic proteins Bcl-xL and Bcl-2 were found to have their expression levels dramatically down-regulated in ESCC cells with propafenone (10 and 20 μ m) treatment. Additionally, propafenone can lower p-ERK expression [3].
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ln Vivo |
Tumor burden was significantly reduced by 69.2% when propafenone (20 mg/kg; intraperitoneally injected every other day) was administered [3]. Additionally, tumor cell proliferation was significantly reduced (average index dropped from 56.3±6.7% in the DMSO-treated group to 20.7±5.1% in the 10 mg/kg propafenone-treated group and from 20.7±5.1% in the 20 mg/kg propafenone-treated group to 11.3±4.0%. treatment group) [3].
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Cell Assay |
Cell proliferation assay[3]
Cell Types: Human esophageal squamous cell carcinoma lines KYSE30, KYSE150 and KYSE270 Tested Concentrations: 5, 10, 15, 20 and 25 μm Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Cells over time Proliferation gradually diminished in KYSE30, KYSE150 and KYSE270 cells, and cell proliferation was effectively inhibited with increasing concentration. Western Blot Analysis [3] Cell Types: Human ESCC cell lines KYSE30, KYSE150 and KYSE270 Tested Concentrations: 0, 10 and 20 μm Incubation Duration: 72 hrs (hours) Experimental Results: A significant down-regulation of Bcl-xL and Bcl-2 expression levels was observed. |
Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (6-8 weeks) carrying KYSE270 xenografts [3]
Doses: 10 mg/kg or 20 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results:Significant effect on tumor growth Inhibitory xenografts. |
References |
[1]. J T Lee, et al. The role of genetically determined polymorphic drug metabolism in the beta-blockade produced by propafenone. N Engl J Med. 1990 Jun 21;322(25):1764-8.
[2]. A Seki, et al. Effects of propafenone on K currents in human atrial myocytes. Br J Pharmacol. 1999 Mar;126(5):1153-62. [3]. Wei-Bin Zheng, et al. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction. Am J Cancer Res. 2017 Nov 1;7(11):2245-2256. |
Molecular Formula |
C21H27NO3
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Molecular Weight |
341.45
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CAS # |
54063-53-5
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Related CAS # |
Propafenone hydrochloride;34183-22-7;(S)-Propafenone;107381-32-8;Propafenone-d7 hydrochloride;1219799-06-0;Propafenone-d5 hydrochloride;1346605-05-7
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SMILES |
CCCNCC(COC1=CC=CC=C1C(=O)CCC2=CC=CC=C2)O
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9287 mL | 14.6434 mL | 29.2869 mL | |
5 mM | 0.5857 mL | 2.9287 mL | 5.8574 mL | |
10 mM | 0.2929 mL | 1.4643 mL | 2.9287 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.