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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPiroxicamCat. No.: HY-B0253CAS No.: 36322-90-4Synonyms: CP-16171分式: CHNOS分量: 331.35作靶点: COX作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (150.90 mM; N
2、eed ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.54 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.54 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/
3、mL (7.54 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Piroxicam (CP-16171)种甾体抗炎剂,能够抑制 COX 的活性,对单核细胞 COX-1 和 COX-2 的 IC50值分别为 47 和 25 M。IC50 & Target COX-2 COX-125 M (IC50, in human monocytes) 47 M (IC50, in human monocytes)体外研究 Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a
4、COX inhibitor, with IC50s of 47,25 M for human monocyte COX-1 and COX-2, respectively 1. Piroxicam (CP-16171) (167, 333, 500 M)decreases cell population of T24 and the 5637 cells. Piroxicam (CP-16171) (500 M) also reduces the cellviability of T24 and 5637 cell, and is significantly effective when co
5、mbined with 0.05 M carboplatin. Thecombination also inhibits Ki-67 expression in booth cells 3.体内研究 Piroxicam (CP-16171) (0.3 mg/kg qd 24-h p.o.) reduces tumor volume in 12 of 18 dogs, and such and effectis via induction of apoptosis and reduction in urine basic fibroblast growth factor concentratio
6、n 2.PROTOCOLCell Assay 3 Urinary bladder cancer cell lines are treated with graded concentrations of carboplatin (0.05, 0.5 and 1 M)and Piroxicam (CP-16171) (167, 333 and 500 M) for 72 h to assess dose-response profiles. For thecombination approach, 0.05 M of carboplatin is used with 333 M Piroxicam
7、. Both drugs are freshlyprepared before each experiment. An untreated control group (cells not exposed to carboplatin andPiroxicam) is used for all assays 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Dogs 2Administration 2 Dogs undergo tumor
8、 staging, including thoracic and abdominal radiography, cystography, ultrasonography,and cystoscopy (with collection of tissue samples) before treatment and after 4 weeks of Piroxicam (CP-16171) (0.3 mg/kg qd 24-h p. o.) treatment. Dogs receive no other cancer treatment during the 4 weeks ofPiroxica
9、m (CP-16171) treatment. Tissue samples are immediately frozen in liquid nitrogen for PGE2 analysisor fixed in 10% neutral buffered formalin for immunohistochemical examination. Urine is also collected beforeand after Piroxicam treatment, aliquoted, and then stored at 80C until analyzed 2.MCE has not
10、 independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kato M, et al. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of non-steroidal anti-inflammatory drugs: investigation using humanperipheral monocytes. J Pharm Pharmacol. 2001 Dec;53(12):1679-85.2/3 Ma
11、ster of Small Molecules 您边的抑制剂师www.MedChemE2. Mohammed SI, et al. Effects of the cyclooxygenase inhibitor, piroxicam, on tumor response, apoptosis, and angiogenesis in a caninemodel of human invasive urinary bladder cancer. Cancer Res. 2002 Jan 15;62(2):356-8.3. Silva J, et al. Synergistic Effect of Carboplatin and Piroxicam on Two Bladder Cancer Cell Lines. Anticancer Res. 2017 Apr;37(4):1737-1745.McePdfHeightCaution: Product has
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