| 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 |
| 运输条件 |
冷藏运输 |
| 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. |
| 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. |
| 规格 |
5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
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英语
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