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Sulindac sulfone
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Sulindac sulfone图片
CAS NO:59864-04-9
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
舒林酸砜是非甾体抗炎药舒林酸的无活性代谢物。
Cas No.59864-04-9
别名磺基舒林,Exisulind
化学名5-fluoro-2-methyl-1-[[4-(methylsulfonyl)phenyl]methylene]-1H-indene-3-acetic acid
Canonical SMILESFC1=CC=C(/C(C(C)=C2CC(O)=O)=C/C3=CC=C(S(C)(=O)=O)C=C3)C2=C1
分子式C20H17FO4S
分子量372.4
溶解度≥ 9.53 mg/mL in DMSO with ultrasonic and warming, ≥ 3.83 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.