BPR1K653 hydrochloride isa potent Aurora kinase inhibitor that inhibits Aurora-A and Aurora-B with IC50 of 24 nM and 45 nM, respectively.
BPR1K653 exhibits less potency (IC50>10 uM) in inhibiting the activity of ALK, CHK1, cMET, EGFR, FLT3, VEGFR1 and VEGFR2.
BPR1K653 induces concentration-dependent decrease in phosphor-Aurora-A, -B and -C kinase in HCT116 cells, inhibits the proliferation of multiple human cancer cell lines regardless of their tissue origins and p53 status (IC50s<0.5 uM).
BPR1K653 shows equal potency in inhibiting the growth of the multiple-drug resistance protein (MDR1) -expressing cancer cells.
BPR1K653 also is effective toward MDR1-expressing tumor xenograft.
