首页
个人中心
委托采购
采购清单

ChemicalBook CAS数据库列表 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE

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

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

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
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

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.