Ensartinib hydrochloride ( X396)

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

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

Related CAS #: 1370651-20-9 (free base) 2137030-98-7 (HCl) 1365267-27-1