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- 详细信息
- 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:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
340267-36-9
- 规格:
50mg/25mg/10mg/5mg
| 规格: | 50mg | 产品价格: | ¥5190.0 |
|---|---|---|---|
| 规格: | 25mg | 产品价格: | ¥3190.0 |
| 规格: | 10mg | 产品价格: | ¥1490.0 |
| 规格: | 5mg | 产品价格: | ¥890.0 |
| 基本信息 | |
| CAS | No.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 |
| 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 |
| MDL | MFCD05863975 |
| SMILES | CS(=O)(=O)C1=CC=C(C=C1)C2=NOC(=C2C3=CC=CC=C3)C(F)(F)F |
| 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. |
| 细胞实验 | 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 |
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文献和实验CDllb 常用单克隆抗体或代号:Mol,OKM1;(Macl,CR3,整合素αM) 主要表达细胞:G,M,T, B, DC, NK,Mac[AS] 分子质量(kDa)和结构:gp170(整合素α) 功 能:iC3b和Fs受体,与ICAM-l和X因子结合,黏附,调理吞噬;结合JAM-3 CDllc 常用单克隆抗体或代号:LeuM乳(CR4.整合素αX) 主要表达细胞:M,G,B
8),又称CR3。作为补体受体,Mae-l通过与Ic3b结合可调理吞噬,在单核细胞和中性粒细胞穿过内皮细胞层迁移到炎症部位时起重要作用。 Mac-1参与PMA诱导的中性粒细胞相互黏附以及趋化作用。表6-2中列举的第3个p2成员是CDllc与CDl8组成的p150-95二聚体(。Xp3),又称CR4。p150-95在CTL杀伤以及中性粒细胞和单核细胞黏附到内皮细胞的过程中起着重要作用,并参与粒细胞的呼吸爆发和B细胞的活化。炎症刺激剂可诱导贮存于胞内颗粒中的p150-95迅速转移
置于培养箱中,不需要拿出培养箱观察,即可对活细胞的行为进行实时、动态、连续地监测,可长达数周,既可得到生长曲线/IC50/EC50,又可生成图片及视频。非常适合免疫学研究中的细胞学实验。 免疫学研究中十大细胞实验: - 基础研究:细胞增殖、免疫分型、免疫细胞激活与分化、细胞健康与凋亡等 - 细胞功能:免疫细胞杀伤、吞噬与清除作用、NETosis等 - 药效评价:趋化/迁移、抗体内化、病毒感染等 Incucyte®实时活细胞分析系统为以上应用与分析提供更高效、更便捷的方案。
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