X-376

Description: X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins, and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. Target: c-Met/HGFR, ALK. Smiles: C[C@@H](Oc1cc(nnc1N)C(=O)Nc1ccc(cc1)C(=O)N1CCN(C)CC1)c1c(Cl)ccc(F)c1Cl. References: Caccese M, et al. Current and developing therapies for the treatment of non-small cell lung cancer with ALK abnormalities: update and perspectives for clinical practice. Expert Opin Pharmacother. 2016 Dec,17(17):2253-2266.