SC-58125
Based on 1 Customer Validation
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. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.92%
- No. CAS: 162054-19-5
- Fòrmula: C17H12F4N2O2S
- Peso molecular:384.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Actividad biológica
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hCOX-2 0.04 μM (IC50) |
hCOX-1 >100 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
>50 μM
Compound: 25
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Inhibitory activity against human recombinant Prostaglandin G/H synthase 1 expressed in microsomes taken from baculovirus infected Sf9 cells
Inhibitory activity against human recombinant Prostaglandin G/H synthase 1 expressed in microsomes taken from baculovirus infected Sf9 cells
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10.1016/0960-894X(95)00564-A |
| Sf9 | IC50 |
0.2 μM
Compound: 25
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Inhibitory activity against human recombinant Prostaglandin G/H synthase 2 expressed in microsomes taken from baculovirus infected Sf9 cells
Inhibitory activity against human recombinant Prostaglandin G/H synthase 2 expressed in microsomes taken from baculovirus infected Sf9 cells
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10.1016/0960-894X(95)00564-A |
| SW982 | IC50 |
33 nM
Compound: SC-58125
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Inhibition of PGE2 release from bradykinin-stimulated human SW982 cells by fluorescence assay
Inhibition of PGE2 release from bradykinin-stimulated human SW982 cells by fluorescence assay
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[PMID: 23581596] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCA-7 and LLC cells
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Concentration:0, 25, 50, 100 μM
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Incubation Time:3 days
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Result:Reduced the cell number and MTT activity in both cell lines in a dose-dependent manner.
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Cell Line:LLC cells
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Concentration:100 μM
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Incubation Time:12 hours
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Result: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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Cell Line:HCA-7 cells
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Concentration:0, 25, 50, 100 μM
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Incubation Time:3 days
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Result:Resulted in a dose-dependent decrease in p34cdc2 activity with strong inhibition, even at the lowest concentration.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic Sprague-Dawley mice are injected HCA-7 cells[3]
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Dosage:10 mg/kg
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Administration:I.p. every 48 h; at the time of tumor implantation or 2 and 4 weeks later
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Result:Decreased the tumor growth rates significantly.
Chemical Information
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No. CAS 162054-19-5
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Appearance Solid
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Peso molecular 384.35
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Fòrmula C17H12F4N2O2S
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Color Off-white to pink
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SMILES
FC(C1=NN(C2=CC=C(S(=O)(C)=O)C=C2)C(C3=CC=C(F)C=C3)=C1)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (650.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gierse JK, et, al. A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors. J Biol Chem. 1996 Jun 28; 271(26): 15810-4. [Content Brief]
[2]. Seibert K, et, al. Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain. Proc Natl Acad Sci U S A. 1994 Dec 6; 91(25): 12013-7. [Content Brief]
[3]. Williams CS, et, al. A cyclooxygenase-2 inhibitor (SC-58125) blocks growth of established human colon cancer xenografts. Neoplasia. Sep-Oct 2001; 3(5): 428-36. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6018 mL | 13.0090 mL | 26.0180 mL | 65.0449 mL |
| 5 mM | 0.5204 mL | 2.6018 mL | 5.2036 mL | 13.0090 mL | |
| 10 mM | 0.2602 mL | 1.3009 mL | 2.6018 mL | 6.5045 mL | |
| 15 mM | 0.1735 mL | 0.8673 mL | 1.7345 mL | 4.3363 mL | |
| 20 mM | 0.1301 mL | 0.6504 mL | 1.3009 mL | 3.2522 mL | |
| 25 mM | 0.1041 mL | 0.5204 mL | 1.0407 mL | 2.6018 mL | |
| 30 mM | 0.0867 mL | 0.4336 mL | 0.8673 mL | 2.1682 mL | |
| 40 mM | 0.0650 mL | 0.3252 mL | 0.6504 mL | 1.6261 mL | |
| 50 mM | 0.0520 mL | 0.2602 mL | 0.5204 mL | 1.3009 mL | |
| 60 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0841 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8131 mL | |
| 100 mM | 0.0260 mL | 0.1301 mL | 0.2602 mL | 0.6504 mL |
SC-58125 Related Classifications
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