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- 文献和实验
- 技术资料
- 保存条件:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
CAY10404
- 库存:
999
- 供应商:
北京索莱宝科技有限公司
- CAS号:
340267-36-9
- 规格:
5mg/10mg/25mg/50mg
| 规格: | 5mg | 产品价格: | ¥890.00 |
|---|---|---|---|
| 规格: | 10mg | 产品价格: | ¥1490.00 |
| 规格: | 25mg | 产品价格: | ¥3190.00 |
| 规格: | 50mg | 产品价格: | ¥5190.00 |
| CAS | 340267-36-9 |
| 英文名称 | CAY10404 |
| 别名 | 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T |
| 分子式 | C17H12F3NO3S |
| 分子量 | 367.34 |
| 规格 | 5mg ; 10mg ; 25mg ; 50mg |
| 溶解性 | Soluble in DMSO ≥1mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| 运输条件 | 冷冻运输 |
| MDL | MFCD05863975 |
| SMILES | CS(=O)(=O)C1=CC=C(C=C1)C2=NOC(=C2C3=CC=CC=C3)C(F)(F)F |
| InChIKey | KKBWWVXRKULXHF-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H12F3NO3S/c1-25(22,23)13-9-7-12(8-10-13)15-14(11-5-3-2-4-6-11)16(24-21-15)17(18,19)20/h2-10H,1H3 |
| PubChem CID | 10429020 |
| 靶点 | COX2;PKB/AKT;MAPK |
| 通路 | Immunology & Inflammation |
| 背景说明 | 是一种有效且高度选择性的COX-2抑制剂,也是有效的 PKB/Akt 和 MAPK 信号通路抑制剂。 |
| 生物活性 | 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[1][2][3]. |
| In Vitro | CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 μM)[1].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[3].CAY10404 (20-100 μM; for 3 days) induces apoptosis in NSCLC cells[3].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[3].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[3].Cell Viability Assay[3]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[3]Cell Line:H460 cells;Concentration:20, 50, 100 μM;Incubation Time:For 3 days;Result: Induced apoptosis.;Western Blot Analysis[3]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. |
| In Vivo | CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury[2].Animal Model: Adult male C57Bl/6J mice weighing 24-30 g[2];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. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|2.7223mL|13.6114mL|27.2227mL|$$|5mM|0.5445mL|2.7223mL|5.4445mL|$$|10mM|0.2722mL|1.3611mL|2.7223mL| |

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