SC 58125

SKU: orb1219266

Description

SC-58125 is a selective cyclooxygenase 2 (COX-2) inhibitor, with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesicSC-58125 treatment on the growth of human colon carcinoma cells in nude mice. Delaying treatment by 2, 4, or 7 weeks following implantation of the carcinoma cells resulted in a significant inhibition of tumor growth. Furthermore, short-term (48 hours) treatment with SC-58125 was sufficient to attenuate tumor growth for up to 15 days. SC-58125 treatment did not alter the rate at which cells underwent apoptosis, but did result in a delayed progression through the cell cycle at the G(2)/M transition. Accordingly, p34(cdc2) protein levels and activity were decreased following SC-58125 treatment.SC-58125 primarily exerts a cytostatic effect in vivo, which is likely to be mediated through inhibition of progression through the G(2)/M phase of the cell cycle.

Key Properties

• CAS Number: 162054-19-5
• MW: 384.35
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂F₄N₂O₂S
• SMILES: FC(C1=NN(C2=CC=C(S(=O)(C)=O)C=C2)C(C3=CC=C(F)C=C3)=C1)(F)F
• Target: COX
• Solubility: DMSO:Soluble

Bioactivity

• In Vivo:
  SC-58125 (10 mg/kg; i.p. every 48 h) inhibits the growth of established colorectal cancer xenografts in mice. SC-58125 (10 mg/kg; a single i.p.) reduces tumor PGE2 levels in mice. SC-58125 (10 mg/kg; a single i.p.) does not change the tumor levels of COX-1 and COX-2 protein in mice. Animal model: Athymic Sprague-Dawley mice are injected HCA-7 cells. Dosage: 10 mg/kg. Administration: i.p. every 48 h; at the time of tumor implantation or 2 and 4 weeks later. Result: Decreased the tumor growth rates significantly.
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• In Vitro:
  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). SC-58125 (10 μM; 20-140 s) is time-dependent and is complete by 1 min, with a half-maximal inhibition at 20 s. SC-58125 (25-100 μM; 3 d) inhibits the in vitro growth of HCA-7 and LLC cells. SC-58125 (100 μM; 12 h) induces G2 arrest in LLC cells. SC-58125 (25-100 μM; 3 d) decreases p34cdc2 levels in HCA-7 cells. SC-58125 (100 μM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells. Cell Proliferation Assay Cell line: HCA-7 and LLC cells. Concentration: 0, 25, 50, 100 μM. Incubation time: 3 days. Result: Reduced the cell number and MTT activity in both cell lines in a dose-dependent manner. Cell Cycle Analysis Cell line: LLC cells. Concentration: 100 μM. Incubation time: 12 hours. Result: Increased in the number of cells containing 4n DNA content in a dose- and time-dependent manner. Reduced the number of mitotic figures. Western blot analysis. Cell line: HCA-7 cells. Concentration: 0, 25, 50, 100 μM. Incubation time: 3 days. Result: Resulted in a dose-dependent decrease in p34cdc2 activity with strong inhibition, even at the lowest concentration.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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Gene Symbol

COX