Sulindac

Catalog No.S2007 Synonyms: MK-231

For research use only.

Sulindac(MK-231) is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.

Sulindac  Chemical Structure

CAS No. 38194-50-2

Selleck's Sulindac has been cited by 8 Publications

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Biological Activity

Description Sulindac(MK-231) is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.
Targets
COX [1]
In vitro

Sulindac and its metabolites sulindac sulfide and sulindac sulfone can also inhibit the NF-kappaB pathway in both colon cancer and other cell lines, due to sulindac-mediated decreases in IKKbeta kinase activity. [1] Sulindac sulfide significantly reduces cell number in both preconfluent and confluent cultures of HT-29 cells with the sulfide showing approximately 4-fold greater potency. Sulindac sulfide inhibits the growth of a variety of tumor cell lines derived from other tissues, as well as normal epithelial cells and fibroblasts. [2] Sulindac sulphide abrogates beta-catenin/TCF-mediated transcription in the CRC cell lines DLD1 and SW480, and decreases the levels of nonphosphorylated beta-catenin. [3]

In vivo

Sulindac not only inhibits tumor formation but decreases small bowel Cox-2 and prostaglandin E(2) to baseline and restored normal levels of apoptosis in a murine modelof familial adenomatous polyposis. [4] Sulindac reduces the tumor number by 95% but does not alter the levels of PGE2 and LTB4 in intestinal tissues in Min/+爉ice. Sulindac reduces tumor number by 82%, whereas eicosanoid levels remained elevates in Min/+ mice. [5] Sulindac causes regression of 70-80% of small intestinal tumors in Min/+ mice within 4 days, but does not have the same impact on colonic lesions. [6]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 356.41
Formula

C20H17FO3S

CAS No. 38194-50-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C2=C(C1=CC3=CC=C(C=C3)S(=O)C)C=CC(=C2)F)CC(=O)O

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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.
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01636128 Withdrawn Drug: difluoromethylornithine|Drug: Sulindac Focus of Study: Drug Response Biomarkers Chemoprevention Neoplasms Cancer Prevention Pharmaceuticals Inc.|University of Arizona March 2014 Phase 2
NCT01843179 Withdrawn Drug: Cytarabine|Drug: Sulindac Acute Myeloid Leukemia Massachusetts General Hospital January 2014 Phase 2
NCT00392665 Terminated Drug: Bevacizumab|Drug: erlotinib|Drug: Sulindac Squamous Cell Carcinoma of the Head and Neck (SCCHN) Massachusetts General Hospital|Dana-Farber Cancer Institute|Emory University|University of North Carolina Chapel Hill|Genentech Inc.|OSI Pharmaceuticals October 2006 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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