Biological Activity of BI 2536:

BI 2536  is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1, derived from human, mouse and rat) (with IC50of 0.83 nM), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations.^[1] Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division.
This compound showed a more than 1000-fold selectivity relative to a panel of 63 other protein kinases, but it also affected the activities of Plk2 at an IC50 of 3.5 nM and, to a slightly lesser extent, the activity of Plk3 (IC50 9.0 nM).^[1]
The half-maximal effective concentration (EC50) values in a panel of 32 human cancer cell lines ranged 2–25 nM.^[1]
BI 2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens.^[1]
 

 

References on BI 2536: