2,5-dimethyl Celecoxib

一种抗癌塞来昔布衍生物；不抑制COX-2（IC50=>100µM）；在HeLa细胞中抑制mPGES-1（IC50=15.6µM）；在HeLa、A549和HCA-7细胞中减少PGE2产生（IC50s=0.64、0.83和3.08µM）；抑制药物敏感的RPMI8226和多药耐药的8226/Dox40多发性骨髓瘤细胞的增殖；在20和30µM的浓度下增加RPMI8226和8226/Dox40细胞的凋亡率；2,5-二甲基塞来昔布的抗增殖效应与mPGES-1抑制无关。An anticancer celecoxib derivative; does not inhibit COX-2 (IC50 = >100 µM); inhibits mPGES-1 in HeLa cells (IC50 = 15.6 µM); reduces PGE2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 µM, respectively); inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226/Dox40 multiple myeloma cells; increases the rate of apoptosis in RPMI8226 and 8226/Dox40 cells at 20 and 30 µM; the antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.