Sulindac

Catalog No.S2007

Sulindac  Chemical Structure

Molecular Weight(MW): 356.41

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

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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  • (d) Parental and regorafenib-resistant HCT116 cells were treated with 40 μM regorafenib, 20 μM sorafenib, 1 μM UCN-01, 1 μM YM-155, 10 μM roscovitine, 15 μM sunitinib, 10 μM crizotinib, 10 nM TRAIL, 10 μM VX680, 20 μM etoposide, 20 μM temsirolimus or 120 μM sulindac sulfide for 48 h. Apoptosis was analyzed as in b. (e) Western blotting of Mcl-1 in parental and regorafenib-resistant HCT116 cells treated with indicated agents as in d for 24 h. Results in (b-d) represent the means±s.d. of three independent experiments. NS, P>0.05; *P<0.05; **P<0.01.

    Oncogene, 2016.. Sulindac purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Sulindac 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

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.2 mM)
Ethanol 9 mg/mL (25.25 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.41
Formula

C20H17FO3S

CAS No. 38194-50-2
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01636128 Withdrawn Focus of Study: Drug Response Biomarkers, Chemoprevention, Neoplasms Cancer Prevention Pharmaceuticals, Inc.|University of Arizona March 2014 Phase 2
NCT01843179 Withdrawn Acute Myeloid Leukemia Massachusetts General Hospital January 2014 Phase 2
NCT01483144 Active, not recruiting Familial Adenomatous Polyposis Cancer Prevention Pharmaceuticals, Inc. October 2013 Phase 3
NCT01856322 Terminated Colorectal Cancer|Liver Metastasis|Colorectal Adenocarcinoma National Cancer Institute (NCI)|Charite University, Berlin, Germany|National Institutes of Health Clinical Center (CC) April 2013 Phase 2
NCT01349881 Recruiting Colorectal Neoplasms Southwest Oncology Group|National Cancer Institute (NCI)|Cancer Prevention Pharmaceuticals, Inc. March 2013 Phase 3
NCT01761877 Recruiting Inflammation|Cancer|Pain|Hypertension Stony Brook University December 2012 Phase 2

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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.

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID