产品描述:
PD 180970 is an inhibitor of Bcr-Abl.{54237} It inhibits wild-type and mutant forms of Bcr-Abl, as well as the p210 isoform, a marker of chronic myelogenous leukemia (CML), with IC50 values ranging from 5 to 48 nM.{54237,54238} PD 180970 is selective for Bcr-Abl over basic FGFR (bFGFR) and PDGFR (IC50s = 934 and 1,430 nM, respectively) but also inhibits Src, LCK, KIT, and EGFR (IC50s = 0.8, 1 phase and apoptosis in K562 CML cells when used at a concentration of 50 nM.{54241} PD 180970 (500 nM) inhibits constitutive STAT3 DNA-binding activity in, and proliferation of, MDA-MB-468 breast cancer cells.{54242} It also inhibits proliferation of Ba/F3 cells expressing mutant p210 Bcr-AblY253F that are resistant to imatinib (Item No. 13139) with an IC50 value of 48 nM.{54238}