Ensartinib (X-396) dihydrochloride is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.
Ensartinib (X-396) dihydrochloride is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM. Ensartinib (X-396) is more potent ALK inhibitors than PF-02341066 (PF-1066). Ensartinib (X-396) potently inhibits H3122 lung cancer cells harboring EML4-ALK E13;A20 (variant 1) with IC50 of 15 nM, 10-fold more potent than PF-02341066. Ensartinib (X-396) display less activity against MET than PF-1066. Ensartinib (X-396) (25mg/kg bid) inhibits tumore growth against H3122 xenografts. Ensartinib (X-396) is effective against multiple ALK variants found in NSCLC, including ALK mutations associated with acquired resistance to PF-1066. Ensartinib (X-396) is synergistic with mTOR inhibitor rapamycin against ALK fusion positive lung cancer cell lines.
