162054-19-5
162054-19-5 structure
- Name: SC-58125
- Chemical Name: sc-58125
- CAS Number: 162054-19-5
- Molecular Formula: C17H12F4N2O2S
- Molecular Weight: 384.348
- Catalog: Signaling Pathways Immunology/Inflammation COX
- Create Date: 2018-06-19 22:46:42
- Modify Date: 2024-01-15 19:43:34
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SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic[1][2][3].
| Name | sc-58125 |
|---|---|
| Synonyms |
5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)pyrazole
1H-Pyrazole, 5-(4-fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)- 5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole 5-(4-fluorophenyl)-1-(4-methylsulfonylphenyl)-3-(trifluoromethyl)pyrazole |
| Description | SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
hCOX-2:0.04 μM (IC50) hCOX-1:>100 μM (IC50) |
| In Vitro | SC-58125 (0.001-100 μM) has a high degree of selectivity for the inducible form of COX-2 (IC50=1 μM) over the COX-1 (IC50>100 μM)[1]. SC-58125 (10 μM; 20-140 s) is time-dependent and is complete by 1 min, with a half-maximal inhibition at 20 s[1]. SC-58125 (25-100 μM; 3 d) inhibits the in vitro growth of HCA-7 and LLC cells[3]. SC-58125 (100 µM; 12 h) induces G2 arrest in LLC cells[3]. SC-58125 (25-100 μM; 3 d) decreases p34cdc2 levels in HCA-7 cells[3]. SC-58125 (100 µM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells[3]. Cell Proliferation Assay[3] 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[3] 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[3] Cell Line: HCA-7 cells Concentration: 0, 25, 50, 100 μM Incubation Time: 3 days Result: Resulted in a dose-dependent decrease in p34cdc2 activity with strong inhibition, even at the lowest concentration. |
| In Vivo | SC-58125 (10 mg/kg; i.p. every 48 h) inhibits the growth of established colorectal cancer xenografts in mice[3]. SC-58125 (10 mg/kg; a single i.p.) reduces tumor PGE2 levels in mice[3]. SC-58125 (10 mg/kg; a single i.p.) does not change the tumor levels of COX-1 and COX-2 protein in mice[3]. Animal Model: Athymic Sprague-Dawley mice are injected HCA-7 cells[3] 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. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 512.6±50.0 °C at 760 mmHg |
| Molecular Formula | C17H12F4N2O2S |
| Molecular Weight | 384.348 |
| Flash Point | 263.8±30.1 °C |
| Exact Mass | 384.055573 |
| PSA | 60.34000 |
| LogP | 3.86 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.573 |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| Hazard Codes | Xi |
| RIDADR | UN 2811 6.1 / PGIII |
| HS Code | 2933199090 |
| HS Code | 2933199090 |
|---|---|
| Summary | 2933199090. other compounds containing an unfused pyrazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |