Description
An inhibitor of wild-type and mutant Bcr-Abl (IC50s = 15 and 9-400 nM, respectively); selective for wild-type and mutant Bcr-Abl over Src and LYN (IC50s = >5,000 nM for both); inhibits Bcr-Abl autophosphorylation and cell proliferation in Ba/F3 cells expressing wild-type or mutant Bcr-Abl (IC50s = 7-155 and 13-51 nM, respectively); reduces midbrain Bcr-Abl autophosphorylation, amyloid-β levels, and neuronal loss, as well as improves autophagosome clearance and reverses cognitive deficits in the Tg2576 transgenic mouse model of Alzheimer’s disease at 1 mg/kg; reduces serum creatine levels, renal profibrotic gene expression, and tubulointerstitial damage, as well as increases survival in a rat model of 5/6 nephrectomy-induced chronic kidney disease