1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
中文名称 | 1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑 |
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中文同义词 | 1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑;5-(4-氟苯基)-1-(4-(甲基磺酰基)苯基)-3-(三氟甲基)-1H-吡唑;化合物SC 58125 |
英文名称 | 1-[(4-METHYLSULFONYL)PHENYL]-3-TRIFLUOROMETHYL-5-(4-FLUOROPHENYL)PYRAZOLE |
英文同义词 | SC-58125;1-[(4-METHYLSULFONYL)PHENYL]-3-TRIFLUOROMETHYL-5-(4-FLUOROPHENYL)PYRAZOLE;5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)pyrazole;5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole;5-(4-Fluoro-phenyl)-1-(4-methanesulfonyl-phenyl)-3-trifluoromethyl-1H-pyrazole;1H-Pyrazole, 5-(4-fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-;Cyclooxygenase,cancer,SC58125,COX,Inhibitor,SC-58125,inflammatory,antitumor,COX-2,edema,inhibit |
CAS号 | 162054-19-5 |
分子式 | C17H12F4N2O2S |
分子量 | 384.35 |
EINECS号 | |
相关类别 | |
Mol文件 | 162054-19-5.mol |
结构式 |
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑 性质
储存条件 | Store at +4°C |
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溶解度 | 二甲基亚砜:≥20mg/mL |
形态 | 粉末 |
颜色 | 白色至类白色 |
hCOX-2 0.04 μM (IC 50 ) |
hCOX-1 >100 μM (IC 50 ) |
SC-58125 (0.001-100 μM) has a high degree of selectivity for the inducible form of COX-2 (IC
50
=1 μM) over the COX-1 (IC
50
>100 μM).
SC-58125 (10 μM; 20-140 s) is time-dependent and is complete by 1 min, with a half-maximal inhibition at 20 s.
SC-58125 (25-100 μM; 3 d) inhibits the in vitro growth of HCA-7 and LLC cells.
SC-58125 (100 µM; 12 h) induces G
2
arrest in LLC cells.
SC-58125 (25-100 μM; 3 d) decreases p34
cdc2
levels in HCA-7 cells.
SC-58125 (100 µM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells.
Cell Proliferation Assay
Cell Line: | HCA-7 and LLC cells |
Concentration: | 0, 25, 50, 100 μM |
Incubation Time: | 3 days |
Result: | Reduced the cell number and MTT activity in both cell lines in a dose-dependent manner. |
Cell Cycle Analysis
Cell Line: | LLC cells |
Concentration: | 100 μM |
Incubation Time: | 12 hours |
Result: |
Increased in the number of cells containing 4n DNA content in a dose- and time-dependent manner.
Reduced the number of mitotic figures. |
Western Blot Analysis
Cell Line: | HCA-7 cells |
Concentration: | 0, 25, 50, 100 μM |
Incubation Time: | 3 days |
Result: | Resulted in a dose-dependent decrease in p34 cdc2 activity with strong inhibition, even at the lowest concentration. |
SC-58125 (10 mg/kg; i.p. every 48 h) inhibits the growth of established colorectal cancer xenografts in mice.
SC-58125 (10 mg/kg; a single i.p.) reduces tumor PGE2 levels in mice.
SC-58125 (10 mg/kg; a single i.p.) does not change the tumor levels of COX-1 and COX-2 protein in mice.
Animal Model: | Athymic Sprague-Dawley mice are injected HCA-7 cells |
Dosage: | 10 mg/kg |
Administration: | I.p. every 48 h; at the time of tumor implantation or 2 and 4 weeks later |
Result: | Decreased the tumor growth rates significantly. |
安全信息
危险品标志 | T |
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危险类别码 | 25 |
安全说明 | 45-24/25-22 |
WGK Germany | 3 |