SC 58125

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SC-58125 是一种选择性环氧合酶 2 (COX-2) 抑制剂，IC50 为 0.04 μM。 SC-58125在体外和体内均表现出抗肿瘤活性，还可以抑制炎症部位的水肿，并对SC-58125治疗裸鼠人结肠癌细胞的生长具有镇痛作用。

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.

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.

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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Chromatin/Epigenetic

COX

COX-2

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162054-19-5

384.35

C17H12F4N2O2S

>98% (HPLC)

DMSO:Soluble

FC(C1=NN(C2=CC=C(S(=O)(C)=O)C=C2)C(C3=CC=C(F)C=C3)=C1)(F)F

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(-20℃)

With Ice Pack

≥ 2 years