| 产品描述： | CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities |
| 靶点： |
COX-2:1 nM (IC50);COX-1:>500 μM (IC50) |
| 体外研究： |
CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 µM). CAY10404 (10-100 µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100 µM. CAY10404 (20-100 µM; for 3 days) induces apoptosis in NSCLC cells. CAY10404 (80 µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β. CAY10404 (20, 50, 80, 100 µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner Cell Viability Assay Cell Line: Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460) Concentration: 10-100 µM Incubation Time: For 3 days Result: Inhibited the growth of NSCLC cell lines in a concentration-dependent manner. Apoptosis Analysis Cell Line: H460 cells Concentration: 20, 50, 100 µM Incubation Time: For 3 days Result: Induced apoptosis. Western Blot Analysis Cell Line: NSCLC cells (H358, H460) Concentration: 80 µM Incubation Time: For 3 days Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels. |
| 体内研究： |
CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury. Animal Model: Adult male C57Bl/6J mice weighing 24-30g Dosage: 50 mg/kg Administration: IP; daily; for 4 days Result: Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α.Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury. |
| 参考文献： |
1. A G Habeeb, et al. Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity. J Med Chem. 2001 Aug 30;44(18):2921-7. 2. Joshua A Robertson, et al. The role of cyclooxygenase-2 in mechanical ventilation-induced lung injury. Am J Respir Cell Mol Biol. 2012 Sep;47(3):387-94. 3. Yongseon Cho, et al. Effects of CAY10404 on the PKB/Akt and MAPK pathway and apoptosis in non-small cell lung cancer cells. Respirology. 2009 Aug;14(6):850-8. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.722 ml |
13.611 ml |
27.223 ml |
| 5 mM |
0.544 ml |
2.722 ml |
5.445 ml |
| 10 mM |
0.272 ml |
1.361 ml |
2.722 ml |
| 50 mM |
0.054 ml |
0.272 ml |
0.544 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京