(E) -Belizatinib

(E) -Belizatinib ((E) -TSR-011) (compound 36) is the (E) -isomer of Belizatinib, and serves as a potent, highly selective, and orally active inhibitor of anaplastic lymphoma kinase (ALK), with an enzymatic IC50 of 0.005 μM and a cellular IC50 of 0.048 μM. The compound exhibits over 61-fold selectivity against JAK2, SRC, and IGF1R, and demonstrates excellent efficacy and pharmacokinetic properties in rats and dogs. (E) -Belizatinib is applicable for research in ALK-driven cancers.