Ensartinib

Description: Ensartinib (formerly known as X-396) is a novel, highly potent and selective, orally available small molecule inhibitor of ALK (anaplastic lymphoma kinase) with an IC50 less than 4 nM in Ambit assays. It is an ALK tyrosine kinase inhibitor (TKI) with additional activity against MET, ABL, Axl, EPHA2, LTK, ROS1 and SLK. ALK autophosphorylation is significantly diminished by ensartinib, albeit at higher concentrations required to block autophosphorylation of the wild-type fusion. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. Therefore, ensartinib has potential anticancer activity.

References: Cancer Res. 2011 Jul 15; 71(14):4920-31.