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3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE

生物活性 靶点 体外研究 体内研究 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE 试剂级价格
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE, 340267-36-9, 结构式
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAS号:
340267-36-9
英文名:
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
英文别名:
CAY10404;3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T;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)-;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
中文名:
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
中文别名:
化合物CAY10404
CBNumber:
CB4355964
分子式:
C17H12F3NO3S
分子量:
367.34
MOL File:
Mol file

3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE化学性质

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
安全信息

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

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.

3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE 上下游产品信息

上游原料

下游产品

3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE 试剂级价格

更新日期产品编号产品名称CAS编号包装价格
2024/04/30HY-1215373-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAY10404		340267-36-95mg900元
2024/04/30HY-1215373-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAY10404		340267-36-910mM * 1mLin DMSO990元

3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE 生产厂家

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340267-36-9, 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE 相关搜索:

  • 抑制剂
  • 对照品
  • 化合物CAY10404
  • 340267-36-9
  • 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
  • 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T
  • Isoxazole, 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-
  • 3-(4-methylsulfonylphenyl)-4-phenyl-5-(trifluoromethyl)-1,2-oxazole
  • 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
  • CAY10404
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