Bcr-abl Inhibitor

Bcr-abl Inhibitor is a cell-permeable pyrimidine compound that binds to and inhibits the c-Abl myristoyl binding pocket. Bcr-abl Inhibitor acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Bcr-abl Inhibitor exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM, nor does it inhibit c-Abl or Bcr-abl in cell-free in vitro kinase assays. Bcr-abl inhibitor exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC₅₀ = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively).