Sulindac Inhibitor CAS No. 38194-50-2

Cat. No.	Name	Size	Price	Add Cart
KI0791	Sulindac	1 g	$60

Chemical Characteristic

Product Name	Sulindac
Synonyms	Clinoril
CAS No.	38194-50-2
Molecular Weight	356.41
Formula	C₂₀H₁₇FO₃S
Chemical Structure

Biological activities

Sulindac is a non-steroidal anti-inflammatory drug of the arylalkanoic acid class. Sulindac is a prodrug that is metabolized into sulindac sulfide and sulindac sulfone. Sulindac sulfide inhibits recombinant human COX-1 and COX-2 with IC50 of 47.9 and 1.2 nM, respectively.^[1] Sulindac sulfide inhibits cyclooxygenase (COX) enzyme activities and suppresses ras-dependent signaling.^[2] In vitro, sulindac and its sulfide and sulfone metabolites all can inhibits the growth of normal human mammary epithelial cell line MCF-10F and human breast cancer cell line MCF-7.^[3] Sulindac can also inhibit the NF-kappaB pathway in both colon cancer and other cell lines. Concentrations of sulindac that inhibit IKKbeta activity also reduce the proliferation of colon cancer cells.^[4] In vivo, sulindac inhibits intestinal tumorigenesis in rodents.^[5] In MiaPaCa-2 xenografts, high-dose sulindac treatment (60 mg/kg) inhibits tumor growth. In BxPC-3 xenografts, low-dose LC-1/sulindac combination treatment (20 mg/kg each) or high-dose sulindac treatment (60 mg/kg) alone significantly reduces tumor size.^[6]

Protocols

In vitro: Sulindac is dissolved in 1 M Tris-HCl, pH 8.0 , to make 1 M stock solution.^[4]

References

[1] Oshima M, et al. Suppression of intestinal polyposis in Apc delta716 knockout mice by inhibition of cyclooxygenase 2 (COX-2). Cell. 1996, 87(5): 803-809. 閵嗏偓閵嗏偓 [2] Taylor MT, et al. Sulindac sulfone inhibits K-ras-dependent cyclooxygenase-2 expression in human colon cancer cells. Cancer Res. 2000, 60(23): 6607-6610. 閵嗏偓閵嗏偓 [3] Han EK, et al. Effects of sulindac and its metabolites on growth and apoptosis in human mammary epithelial and breast carcinoma cell lines. Breast Cancer Res Treat. 1998, 48(3): 195-203. [4] Yamamoto Y, et al. Sulindac inhibits activation of the NF-kappaB pathway. J Biol Chem. 1999, 274(38): 27307-27314. 閵嗏偓閵嗏偓 [5] Yang W, et al. p21(WAF1/cip1) is an important determinant of intestinal cell response to sulindac in vitro and in vivo. Cancer Res. 2001, 61(16): 6297-6302. 閵嗏偓閵嗏偓 [6] Yip-Schneider MT, et al. Suppression of pancreatic tumor growth by combination chemotherapy with sulindac and LC-1 is associated with cyclin D1 inhibition in vivo. Mol Cancer Ther. 2007, 6(6): 1736-1744. 閵嗏偓閵嗏偓

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