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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1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑 用途与合成方法
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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. |
