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SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $33 | In Stock | |
5 mg | $52 | In Stock | |
10 mg | $93 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $252 | In Stock | |
100 mg | $323 | In Stock | |
1 mL x 10 mM (in DMSO) | $58 | In Stock |
Description | SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors. |
Targets&IC50 | COX-1:9 nM. |
In vitro | Preincubation of cyclooxygenase-1 (COX-1) with SC-560 selectively inhibits the conversion of arachidonic acid to prostaglandin E2 (PGE2) in a concentration-dependent manner, demonstrating higher specificity for COX-1 over COX-2, as indicated by SC-560's inhibitory concentration 50 (IC50) for COX-2 being 6.3 μM, nearly 1,000-fold greater than for COX-1. Furthermore, SC-560 has been shown to suppress hepatocellular carcinoma (HCC) cell growth, colony formation in soft agar, and induce apoptosis in a dose- and time-dependent manner. Additionally, it downregulates anti-apoptotic proteins, including survivin and X-linked inhibitor of apoptosis protein (XIAP), while simultaneously activating caspases 3 and 7, illustrating its therapeutic potential in HCC treatment through multifaceted mechanisms of action. |
In vivo | Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2 production, indicating that SC-560 is orally bioavailable and inhibits COX-1 in vivo. SC-560 extensively distributes into rat tissues, with a CL approaching hepatic plasma flow. However, after oral administration, it exhibits low (<15%), formulation-dependent bioavailability and demonstrates kidney toxicity. |
Kinase Assay | Test compound is incubated with human whole blood stimulated with bacterial LPS for 4 h, followed by capture of MPO on immobilized anti-MPO antibody coated plates. The captured MPO is washed and residual MPO activity is determined using Amplex Red and H2O2. |
Cell Research | SC-560 is dissolved in DMSO[2].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. |
Animal Research | Rat: 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. |
Alias | SC560 |
Molecular Weight | 352.74 |
Formula | C17H12ClF3N2O |
Cas No. | 188817-13-2 |
Smiles | COc1ccc(cc1)-n1nc(cc1-c1ccc(Cl)cc1)C(F)(F)F |
Relative Density. | 1.33g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 35.3 mg/mL (100.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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