Sulindac sulfone
(Synonyms: 磺基舒林,Exisulind) 目录号 : GC11721
A metabolite of sulindac
Cas No.:59864-04-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 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 SMILES | FC1=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。