Sulindac sulfone (Synonyms: Exisulind) |
| Catalog No.GC11721 |
Sulindac sulfone is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59864-04-9
Sample solution is provided at 25 µL, 10mM.
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Sulindac sulfone is a metabolite of the nonsteroidal anti-inflammatory drug (NSAID) sulindac.
In vitro: Sulindac sulfone treatment also inhibited PGE2 production by HCA-7 cells with an IC50 of 360 mmol/L. Sulindac sulfone at 100 mmol/L reduced 6-ketoPGFα by 29.2%. Sulindac sulfone reduced the colony number of HCA-7 and HCT-116 with an EC50 of 50 mmol/l[1]. Sulindac sulfone significantly decreased the expression of total cellular β-catenin (50% of control), pro-caspase 3 (49%), cyclin D1 (51%), and PPARδ (65%) in SW480 cells. No significant alteration in pro-caspase 3 or β-catenin expression was found in HCA7, LS174, or Caco-2 cells treated with sulindac sulfone. A dose-dependent reduction in TCF-mediated transcriptional activity was also observed in SW480 cells [2].
In vivo: Sulindac sulfone is capable of reducing the incidence, multiplicity and tumor burden in the azoxymethane AOM rat model of colorectal cancer. Sulindac sulfone had no effect on the growth of HCA-7, HCT-116 xenografts and cancer cell xenografts [1].
Clinical Trial: In patients with familial adenomatous polyposis, treatment of sulindac sulfone for a period of six months led to regression of small polyps [3].
References:
[1] Williams C S, Goldman A P, Sheng H, et al. Sulindac sulfide, but not sulindac sulfone, inhibits colorectal cancer growth[J]. Neoplasia, 1999, 1(2): 170-176.
[2] CHANG W E N C H I L, Everley L C, Pfeiffer G R, et al. Sulindac Sulfone Is Most Effective in Modulating β‐Catenin‐Mediated Transcription in Cells with Mutant APC[J]. Annals of the New York Academy of Sciences, 2005, 1059(1): 41-55.
[3] Stoner G D, Budd G T, Ganapathi R, et al. Sulindac sulfone induced regression of rectal polyps in patients with familial adenomatous polyposis[M]//Colon Cancer Prevention. Springer US, 1999: 45-53.
| Cas No. | 59864-04-9 | SDF | |
| Synonyms | Exisulind | ||
| Chemical Name | 5-fluoro-2-methyl-1-[[4-(methylsulfonyl)phenyl]methylene]-1H-indene-3-acetic acid | ||
| Canonical SMILES | FC1=CC=C(/C(C(C)=C2CC(O)=O)=C/C3=CC=C(S(C)(=O)=O)C=C3)C2=C1 | ||
| Formula | C20H17FO4S | M.Wt | 372.4 |
| Solubility | ≥ 9.53 mg/mL in DMSO with ultrasonic and warming, ≥ 3.83 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6853 mL | 13.4264 mL | 26.8528 mL |
| 5 mM | 0.5371 mL | 2.6853 mL | 5.3706 mL |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6853 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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