PIM program
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Highly potent PIM-1,2,3 inhibitors for partnering or development
PIM Kinases
PIM family kinases (PIMs 1, 2 and 3) are the driving force behind excessive proliferation in numerous types of cancer and they represent validated drug targets in many hematologic cancers and select solid tumors. Because PIM kinases share many of the same substrates as kinases of the Akt pathway, a PIM inhibitor is well positioned for combination therapy with inhibitors of the Akt pathway. The overlapping and compensatory nature of PIM-1 and PIM-2 highlight the importance of inhibiting all isoforms with a pan-PIM kinase inhibitor. Toward this goal, Cylene has created multiple, proprietary chemical series in which selective inhibition of all three PIM kinases can be achieved in the low nM to pM range and the inhibitory activity against other kinases can be dialed in or out as desired.
Pan-PIM Kinase Inhibitors
Cylene has created four unique chemical scaffolds as pan-PIM inhibitors, and representative molecules from these scaffolds inhibit PIM-1, PIM-2 and PIM-3 in the low nanomolar to picomolar range while exhibiting no inhibitory activity of the FLT3 protein kinase. The in vivo and in vitro profiles of these chemically diverse series are indicative of an effective and potent anticancer mechanism mediated through the selective inhibition of PIM kinases. Cylene’s unique chemistry and experience in the development of serine/threonine kinase inhibitors has driven the development of multiple proprietary chemical series of pan-PIM inhibitors exhibiting picomolar potency and discerning selectivity.
