188817-13-2
188817-13-2 structure
- Name: SC-560
- Chemical Name: 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)pyrazole
- CAS Number: 188817-13-2
- Molecular Formula: C17H12ClF3N2O
- Molecular Weight: 352.738
- Catalog: Research Areas Cancer
- Create Date: 2018-11-22 20:15:16
- Modify Date: 2024-01-02 12:41:56
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SC-560 is a potent and selective COX-1 inhibitor with an IC50 of 9 nM.
| Name | 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)pyrazole |
|---|---|
| Synonyms |
Ionomycin calcium salt
Lopac-S-2064 5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole 1H-Pyrazole, 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)- 5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethyl pyrazole SC560 SC-560 |
| Description | SC-560 is a potent and selective COX-1 inhibitor with an IC50 of 9 nM. |
|---|---|
| Related Catalog | |
| Target |
COX-1:9 nM (IC50) COX-2:6.3 μM (IC50) |
| In Vitro | Preincubation of COX-1 with SC-560 inhibits the conversion of arachidonic acid to PGE2 in a concentration-dependent manner. The IC50 of SC-560 for COX-2 is 6.3 μM, nearly 1,000-fold higher than with COX-1[1]. SC-560 shows a dose and time dependent inhibitory effect on HCC cell growth. SC-560 also inhibits colony formation in soft agar and induces apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreases the levels of the anti-apoptotic proteins survivin and XIAP and activates caspase 3 and 7 in a dose and time dependent fashion[2]. |
| In Vivo | Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2production, indicating that SC-560 is orally bioavailable and inhibits COX-1 in vivo[1]. SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. The drug displays low less than 15% and formulation dependent bioavailability after oral administration and demonstrates kidney toxicity[3]. |
| Cell Assay | HuH-6 and HA22T/VGH cells (5000/well) are treated with various concentrations of SC-560 (5, 10, 25, 50, 100, 200 μM) and cultured for 72 h. At the end of treatment, cell viability is assessed by MTS assay[2]. |
| Animal Admin | Rats: The pharmacokinetics of SC-560 is studied in Sprague-Dawley rats after a single intravenous (i.v.) and oral dose (10 mg/kg) in polyethylene glycol (PEG) 600 and a single oral dose (10 mg/kg) in 1% methylcellulose (MC). Serial blood samples are collected via a catheter inserted in the right jugular vein and serum samples are analysed for SC-560 using reverse phase HPLC. After oral administration of SC-560 in PEG, urine is also collected for 24 h and analyzed for urinary sodium, chloride, and potassium as well as NAG[3]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 440.6±45.0 °C at 760 mmHg |
| Melting Point | 63 °C |
| Molecular Formula | C17H12ClF3N2O |
| Molecular Weight | 352.738 |
| Flash Point | 220.3±28.7 °C |
| Exact Mass | 352.059021 |
| PSA | 27.05000 |
| LogP | 6.13 |
| Vapour Pressure | 0.0±1.0 mmHg at 25°C |
| Index of Refraction | 1.564 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xi: Irritant; |
| Risk Phrases | R36/37/38 |
| Safety Phrases | 26-36 |
| RIDADR | NONH for all modes of transport |
| HS Code | 2933199090 |
| Precursor 3 | |
|---|---|
| DownStream 0 | |
| 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% |