Definition

An orally available small molecule pan-inhibitor of the PIM serine/threonine kinase family, with potential antineoplastic activity. Upon oral administration, pan-PIM kinase inhibitor GDC-0570 binds to and prevents the activation of the three PIM family kinases, PIM1, PIM2 and PIM3. This prevents the activation of PIM-mediated signaling pathways and inhibits proliferation in cells that overexpress PIMs. PIMs, constitutively active proto-oncogenic serine/threonine kinases upregulated in various types of cancers, play key roles in tumor cell proliferation and survival.