Sulindac sulfone

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Chemical Structure| 59973-80-7 同义名 : -
CAS号 : 59973-80-7
货号 : A1161164
分子式 : C20H17FO4S
纯度 : 97%
分子量 : 372.41
MDL号 : MFCD00871143
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Sulindac sulfone is a metabolite of sulindac, a non-steroidal anti-inflammatory drug (NSAID), without anti-inflammatory ability. VDAC1 and VDAC2 (voltage-dependent anion channel) are direct targets of sulindac sulfone which suppresses the mTORC1 pathway and induces G1 arrest[1]. At 100 microMol of sulindac sulfone, a decrease in beta-catenin concentration of 5% was observed; increasing concentrations of sulindac sulfone resulted in >70% reduction in secreted beta-catenin. Sulindac sulfone reduced levels of secreted beta-catenin in the HNSCC (head and neck squamous cell carcinoma) cell line UM-SCC 11A after 48 hours of incubation[2]. Sulindac sulfone inhibited COX-2 (cyclooxygenase) protein expression, which resulted in a decrease in prostaglandin synthase E2 production[3]. Sulindac (20 mg/kg/day), sulindac sulfone (40 mg/kg/day), or vehicle was administered orally to male Sprague-Dawley rats for a 4-wk period beginning 20 wk after tumor induction. Sulindac and sulindac sulfone treatment significantly reduced the number and volume of colorectal tumors compared with control rats[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.43mL

2.69mL

1.34mL

26.85mL

5.37mL

2.69mL

参考文献

[1]Aono Y, Horinaka M, Iizumi Y, Watanabe M, Taniguchi T, Yasuda S, Sakai T. Sulindac sulfone inhibits the mTORC1 pathway in colon cancer cells by directly targeting voltage-dependent anion channel 1 and 2. Biochem Biophys Res Commun. 2018 Nov 10;505(4):1203-1210

[2]Sauter A, Soulsby H, Hormann K, Naim R. Sulindac sulfone induces a decrease of beta-catenin in HNSCC. Anticancer Res. 2010 Feb;30(2):339-43

[3]Taylor MT, Lawson KR, Ignatenko NA, Marek SE, Stringer DE, Skovan BA, Gerner EW. Sulindac sulfone inhibits K-ras-dependent cyclooxygenase-2 expression in human colon cancer cells. Cancer Res. 2000 Dec 1;60(23):6607-10

[4]de Jong TA, Skinner SA, Malcontenti-Wilson C, Vogiagis D, Bailey M, van Driel IR, O'Brien PE. Inhibition of rat colon tumors by sulindac and sulindac sulfone is independent of K-ras (codon 12) mutation. Am J Physiol Gastrointest Liver Physiol. 2000 Feb;278(2):G266-72