Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies
Fig 2
INCB053914 inhibits cellular proliferation in hematologic tumor cell lines (A), inhibits phosphorylation of PIM substrates (B), including pBAD (C), and increases PIM2 expression (D) in hematologic tumor cell lines. For all Western blots, actin controls confirmed equivalent loading. IC50 values for pBAD inhibition were determined by fitting the percent inhibition versus the log [INCB053914] data to sigmoidal dose–response (variable slope) curve. Error bars represent standard deviation. GI50 values >3 μM are not shown. *pP70S6K band intensities in KMS-12-BM (MM) cells were below the limit of detection at all INCB053914 concentrations tested. HL, Hodgkin lymphoma; ND, not determined. Original Western blot images are shown in Supporting Information S4 File.