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| 5mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
SC-560 is a novel, potent,orally bioavailable and selective COX-1 (cyclooxygenase-1) inhibitor with an IC50 of 9 nM. SC-560 inhibited colony formation in soft agar and induced apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreased the levels of the anti-apoptotic proteins survivin and XIAP and activated caspase-3 and -7 in a dose- and time-dependent fashion. SC-560 exhibits anti-tumor and apoptotic effects in human HCC cells. SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. The drug displays low<15% and formulation dependent bioavailability after oral administration and demonstrates kidney toxicity.
| ln Vitro |
In a concentration-dependent manner, the pre-dilution of COX-1 and SC-560 prevents arachidonic acid from being converted to PGE2. Compared to COX-1, SC-560 has an IC50 of 6.3 μM against COX-2, which is about 1,000 times greater[1]. SC-560 shows dose- and time-dependent suppression of the development of HCC cells. In soft agar, SC-560 also prevents colony formation and stimulates dose-dependent HCC cell proliferation. Furthermore, in a manner that is dependent on both dose and time, SC-560 activates caspases 3 and 7 and decreases the amounts of the anti-tumor cell growth sudan proteins Svivin and XIAP [2].
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| ln Vivo |
Ionophore-stimulated TxB2 production was totally suppressed by injury of 10 or 30 mg/kg SC-560 1 hour prior to test, suggesting that SC-560 has biolesion availability and inhibits COX-1 in vivo [1]. In the scaffold tissue, SC-560 was extensively dispersed, and CL was in close proximity to the hepatic venous flow. The medication shows nephrotoxicity, limited bioavailability, and formulation dependence of less than 15% following epidermal formulation [3].
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| References |
[1]. Smith CJ, et al. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13313-8.
[2]. Lampiasi N, et al. The selective cyclooxygenase-1 inhibitor SC-560 suppresses cell proliferation and induces apoptosis in human hepatocellular carcinoma cells. Int J Mol Med. 2006 Feb;17(2):245-52. [3]. Teng XW, et al. Formulation dependent pharmacokinetics, bioavailability and renal toxicity of a selective cyclooxygenase-1 inhibitor SC-560 in the rat. J Pharm Pharm Sci. 2003 May-Aug;6(2):205-10 |
| Molecular Formula |
C17H12CLF3N2O
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|---|---|
| Molecular Weight |
352.7382
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| CAS # |
188817-13-2
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| SMILES |
FC(C1=NN(C2=CC=C(OC)C=C2)C(C3=CC=C(Cl)C=C3)=C1)(F)F
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| InChi Key |
PQUGCKBLVKJMNT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12ClF3N2O/c1-24-14-8-6-13(7-9-14)23-15(10-16(22-23)17(19,20)21)11-2-4-12(18)5-3-11/h2-10H,1H3
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| Chemical Name |
5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
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| Synonyms |
SC-560; SC 560; SC560.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~283.49 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8349 mL | 14.1747 mL | 28.3495 mL | |
| 5 mM | 0.5670 mL | 2.8349 mL | 5.6699 mL | |
| 10 mM | 0.2835 mL | 1.4175 mL | 2.8349 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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