3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
- CAS号:340267-36-9
- 英文名:3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
- 中文名:3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
- CBNumber:CB4355964
- 分子式:C17H12F3NO3S
- 分子量:367.34
- MOL File:Mol file
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:100.0(Max Conc. mg/mL);272.23(Max Conc. mM)
- 形态 :A crystalline solid
- 颜色 :White to off-white
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE性质、用途与生产工艺
- 生物活性 CAY10404 是一种有效且高度选择性的环氧合酶 2 (COX-2) 抑制剂，IC50 为 1 nM，选择性指数 (SI；COX-1 IC50/COX-2 IC50) 为 >500000。CAY10404 是有效的 PKB/Akt 和 MAPK 信号通路抑制剂，可诱导非小细胞肺癌 (NSCLC) 细胞凋亡 (apoptosis)。CAY10404 是一种二芳基异恶唑，具有良好的止痛，抗炎和抗癌活性。
-
靶点
COX-2
1 nM (IC 50 )
COX-1
>500 μM (IC 50 )
Akt
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体外研究
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. -
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 24-30 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.
- 更新日期：2024/11/08
- 产品编号：HY-121537
- 产品名称：3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE CAY10404
- CAS编号：340267-36-9
- 包装：5mg
- 价格：900元
- 更新日期：2024/11/08
- 产品编号：HY-121537
- 产品名称：3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE CAY10404
- CAS编号：340267-36-9
- 包装：10mM * 1mLin DMSO
- 价格：990元
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