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.
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.