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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- CAS号:
- 162054-19-5
- 英文名:
- 1-[(4-METHYLSULFONYL)PHENYL]-3-TRIFLUOROMETHYL-5-(4-FLUOROPHENYL)PYRAZOLE
- 英文别名:
- SC-58125;1-[(4-METHYLSULFONYL)PHENYL]-3-TRIFLUOROMETHYL-5-(4-FLUOROPHENYL)PYRAZOLE;5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)pyrazole;5-(4-Fluoro-phenyl)-1-(4-methanesulfonyl-phenyl)-3-trifluoromethyl-1H-pyrazole;5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)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
- 中文名:
- 1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
- 中文别名:
- 化合物SC 58125;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
- CBNumber:
- CB6486473
- 分子式:
- C17H12F4N2O2S
- 分子量:
- 384.35
- MOL File:
- 162054-19-5.mol
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1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑化学性质
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储存条件:
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Store at +4°C
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溶解度:
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DMSO: ≥20mg/mL
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形态:
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powder
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颜色:
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white to off-white
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1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑性质、用途与生产工艺
SC-58125 是一种有效的和选择性的环氧合酶 2 (COX-2) 的抑制剂，IC50 值为 0.04 μM。SC-58125 在体外和体内均表现出抗肿瘤活性，还可以抑制炎症部位的水肿并具有镇痛作用。
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hCOX-2
0.04 μM (IC
50
)
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hCOX-1
>100 μM (IC
50
)
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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
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Cell Line:
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HCA-7 and LLC cells
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Concentration:
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0, 25, 50, 100 μM
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Incubation Time:
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3 days
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Result:
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Reduced the cell number and MTT activity in both cell lines in a dose-dependent manner.
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Cell Cycle Analysis
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Cell Line:
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LLC cells
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Concentration:
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100 μM
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Incubation Time:
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12 hours
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Result:
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Increased in the number of cells containing 4n DNA content in a dose- and time-dependent manner.
Reduced the number of mitotic figures.
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Western Blot Analysis
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Cell Line:
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HCA-7 cells
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Concentration:
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0, 25, 50, 100 μM
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Incubation Time:
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3 days
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Result:
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Resulted in a dose-dependent decrease in p34
cdc2
activity with strong inhibition, even at the lowest concentration.
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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.
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Animal Model:
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Athymic Sprague-Dawley mice are injected HCA-7 cells
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Dosage:
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10 mg/kg
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Administration:
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I.p. every 48 h; at the time of tumor implantation or 2 and 4 weeks later
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Result:
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Decreased the tumor growth rates significantly.
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1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
上下游产品信息
上游原料
下游产品
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
生产厂家
162054-19-5, 1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑 相关搜索:
- C17H12F4N2O2S
- 化合物SC 58125
- 5-(4-氟苯基)-1-(4-(甲基磺酰基)苯基)-3-(三氟甲基)-1H-吡唑
- 1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
- 162054-19-5
- Cyclooxygenase,cancer,SC58125,COX,Inhibitor,SC-58125,inflammatory,antitumor,COX-2,edema,inhibit
- 1H-Pyrazole, 5-(4-fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-
- 5-(4-Fluoro-phenyl)-1-(4-methanesulfonyl-phenyl)-3-trifluoromethyl-1H-pyrazole
- 5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole
- 5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)pyrazole
- 1-[(4-METHYLSULFONYL)PHENYL]-3-TRIFLUOROMETHYL-5-(4-FLUOROPHENYL)PYRAZOLE
- SC-58125