product name Sulindac
Description: Sulindac belongs to the arylalkanoic acid class, and is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, it is used in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in the body to the active NSAID, sulindac sulfide, a cyclooxgenase inhibitor that represses ras signaling, and sulindac sulfone, an antitumor agent, following oral administration in vivo.
References: J Biol Chem. 1999 Sep 17;274(38):27307-14; Cancer Res. 1997 Oct 1;57(19):4267-73.
356.41
Formula
C20H17FO3S
CAS No.
38194-50-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 71 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 9 mg/mL (25.25 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19406962
| In Vitro |
In vitro activity: 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. 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. Sulindac sulphide abrogates beta-catenin/TCF-mediated transcription in the CRC cell lines DLD1 and SW480, and decreases the levels of nonphosphorylated beta-catenin. Kinase Assay: Cell Assay: |
|---|---|
| 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. Sulindac reduces the tumor number by 95% but does not alter the levels of PGE2 and LTB4 in intestinal tissues in mice. Sulindac reduces tumor number by 82%, whereas eicosanoid levels remained elevates in Min/+ mice. |
| Animal model | |
| Formulation & Dosage | |
| References | J Biol Chem. 1999 Sep 17;274(38):27307-14; Cancer Res. 1996 Jun 1;56(11):2556-60; Cancer Res. 1997 Oct 1;57(19):4267-73. |
