| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| ln Vitro |
High selectivity for inducible COX-2 (IC50=1 μM) over COX-1 (IC50>100 μM) is exhibited by SC-58125 (0.001-100 μM) [1]. Time-dependent, SC-58125 (10 μM; 20-140 seconds) reaches half-maximal inhibition at 20 seconds and completes inhibition in 1 minute [1]. In vitro, SC-58125 (25-100 μM; 3 d) suppresses the development of LLC and HCA-7 cells [3]. In LLC cells, SC-58125 (100 µM; 12 hours) causes G2 arrest [3]. In HCA-7 cells, SC-58125 (25-100 μM; 3 d) lowers p34cdc2 levels [3]. In HCA-7 and LLC cells, SC-58125 (100 µM; 24 or 72 hours) does not cause apoptosis [3].
|
|---|---|
| ln Vivo |
Established colorectal cancer xenografts in mice are inhibited in growth by SC-58125 (10 mg/kg; intraperitoneally every 48 hours) [3]. In mice, tumor PGE2 levels can be decreased by SC-58125 (10 mg/kg; single intraperitoneal injection) [3]. Mice's tumor levels of COX-1 and COX-2 proteins are unaffected by SC-58125 (10 mg/kg; single intraperitoneal injection) [3].
|
| Cell Assay |
Cell proliferation assay[3]
Cell Types: HCA-7 and LLC Cell Tested Concentrations: 0, 25, 50, 100 μM Incubation Duration: 3 days Experimental Results: Cell number and MTT activity were diminished in a dose-dependent manner in both cell lines . Cell cycle analysis[3] Cell Types: LLC Cell Tested Concentrations: 100 μM Incubation Duration: 12 hrs (hours) Experimental Results: The number of cells containing 4n DNA content increased in a dose- and time-dependent manner. Mitotic numbers are diminished. Western Blot Analysis[3] Cell Types: HCA-7 Cell Tested Concentrations: 0, 25, 50, 100 μM Incubation Duration: 3 days Experimental Results: Even at the lowest concentration, a dose-dependent decrease in p34cdc2 activity was induced with a strong inhibitory effect. |
| Animal Protocol |
Animal/Disease Models: Athymic SD (SD (Sprague-Dawley)) mice injected with HCA-7 cells [3]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection every 48 hrs (hrs (hours)); at the time of tumor implantation or after 2 and 4 weeks. Experimental Results: significant Dramatically reduce tumor growth rate. Carrageenan-induced paw edema and hyperalgesia: Male Sprague-Dawley rats were used. SC-58125 was suspended in 0.5% methylcellulose in water and administered orally by gavage 1 hour prior to carrageenan injection (0.1 ml of 1% carrageenan in saline into the hindpaw). Paw volume was measured at intervals to assess edema. Hyperalgesia was measured as the withdrawal latency to a radiant heat source applied to the hindpaw. Measurements were taken 3 hours after carrageenan injection. [2] Rat air pouch model: An air cavity was produced by subcutaneous injection of sterile air into the back of male rats. Carrageenan (1% solution) was injected into the pouch. Animals were fasted for 17 hours and then pretreated with SC-58125 (0.001 – 10 mg/kg, orally) 1 hour prior to carrageenan administration. After 6 hours, pouch exudates were collected for prostaglandin determination. Stomachs were excised for visual examination of gastric glandular damage and processed for tissue prostaglandin production. [2] Gastric toxicity study: Rats were fasted for 16 hours prior to administration of SC-58125 (0.03 – 30 mg/kg) by gavage. Five hours after administration, stomachs were removed and inspected for gastric glandular mucosal damage with a stereomicroscope. No visible gastric lesions were observed at doses up to 400 mg/kg (60 times the ED₅₀ for edema). [2] Intestinal toxicity study: Fed rats were dosed once with a suspension of SC-58125 (400 or 600 mg/kg) intragastrically. After 72 hours, animals were euthanized, and the abdominal cavity was opened to assess the presence of adhesions. No intestinal lesions were observed at doses up to 200 mg/kg. [2] |
| References |
|
| Additional Infomation |
SC-58125 is a pyrazole compound with the structure 1H-pyrazole, substituted at the 5-position with a 4-fluorophenyl group, at the 1-position with a 4-(methanesulfonyl)phenyl group, and at the 3-position with a trifluoromethyl group. It is a selective cyclooxygenase-2 inhibitor with anticancer activity. It can be used as both a cyclooxygenase-2 inhibitor and an antitumor drug. SC-58125 belongs to the pyrazole class, organofluorine compounds, and sulfone class of compounds.
|
| Molecular Formula |
C17H12N2O2F4S
|
|---|---|
| Molecular Weight |
384.34798
|
| Exact Mass |
384.055
|
| CAS # |
162054-19-5
|
| PubChem CID |
115239
|
| Appearance |
Off-white to pink solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
512.6±50.0 °C at 760 mmHg
|
| Flash Point |
263.8±30.1 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.573
|
| LogP |
3.86
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
26
|
| Complexity |
577
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CS(=O)(=O)C1=CC=C(C=C1)N2C(=CC(=N2)C(F)(F)F)C3=CC=C(C=C3)F
|
| InChi Key |
JHBIMJKLBUMNAU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H12F4N2O2S/c1-26(24,25)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
|
| Chemical Name |
5-(4-fluorophenyl)-1-(4-methylsulfonylphenyl)-3-(trifluoromethyl)pyrazole
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~650.45 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6018 mL | 13.0090 mL | 26.0180 mL | |
| 5 mM | 0.5204 mL | 2.6018 mL | 5.2036 mL | |
| 10 mM | 0.2602 mL | 1.3009 mL | 2.6018 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.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
