Bioactivity | SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect[1][2][3]. |
Invitro | 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)[1].SC-58125 (10 μM; 20-140 s) is time-dependent and is complete by 1 min, with a half-maximal inhibition at 20 s[1].SC-58125 (25-100 μM; 3 d) inhibits the in vitro growth of HCA-7 and LLC cells[3].SC-58125 (100 µM; 12 h) induces G2 arrest in LLC cells[3].SC-58125 (25-100 μM; 3 d) decreases p34cdc2 levels in HCA-7 cells[3].SC-58125 (100 µM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells[3]. Cell Proliferation Assay[3] Cell Line: |
In Vivo | SC-58125 (10 mg/kg; i.p. every 48 h) inhibits the growth of established colorectal cancer xenografts in mice[3].SC-58125 (10 mg/kg; a single i.p.) reduces tumor PGE2 levels in mice[3].SC-58125 (10 mg/kg; a single i.p.) does not change the tumor levels of COX-1 and COX-2 protein in mice[3]. Animal Model: |
Name | SC-58125 |
CAS | 162054-19-5 |
Formula | C17H12F4N2O2S |
Molar Mass | 384.35 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Gierse JK, et, al. A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors. J Biol Chem. 1996 Jun 28; 271(26): 15810-4. [2]. Seibert K, et, al. Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain. Proc Natl Acad Sci U S A. 1994 Dec 6; 91(25): 12013-7. [3]. Williams CS, et, al. A cyclooxygenase-2 inhibitor (SC-58125) blocks growth of established human colon cancer xenografts. Neoplasia. Sep-Oct 2001; 3(5): 428-36. |