3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
中文名称 | 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE |
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中文同义词 | 化合物CAY10404 |
英文名称 | 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE |
英文同义词 | CAY10404;3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE;3-(4-methylsulfonylphenyl)-4-phenyl-5-(trifluoromethyl)-1,2-oxazole;Isoxazole, 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-;3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T;Bcl-XL,CAY10404,cancer,COX,anti-inflammatory,Bcl-2,Apoptosis,Akt,H-1703,Cyclooxygenase,NSCLC,CAY 10404,H-358,inhibit,cell,pGSK-3β,H-460,analgesic,MAPK,CAY-10404,cyclooxygenase-2,lung,anti-cancer,Inhibitor,Non-small,Protein kinase B,pAkt,PKB |
CAS号 | 340267-36-9 |
分子式 | C17H12F3NO3S |
分子量 | 367.34 |
EINECS号 | |
相关类别 | 对照品 |
Mol文件 | Mol File |
结构式 |
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE 性质
储存条件 | Store at -20°C |
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溶解度 | DMSO:100.0(最大浓度 mg/mL);272.23(最大浓度 mM) |
形态 | 结晶固体 |
颜色 | 白色至米白色 |
COX-2 1 nM (IC 50 ) |
COX-1 >500 μM (IC 50 ) |
Akt
|
CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC
50
>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 (IC
50
) 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-X
L
) 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-X L ) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels. |
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 24-30 g |
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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-121537 | 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE CAY10404 | 340267-36-9 | 5mg | 900元 |
2024/08/19 | HY-121537 | 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE CAY10404 | 340267-36-9 | 10mM * 1mLin DMSO | 990元 |