Ensartinib (X-396) dihydrochloride (C09-0881-180)

InformationEnsartinib (X-396) dihydrochloride Ensartinib (X-396) is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM.TargetsTPM3-TRKA (Cell-free assay); TRKC (Cell-free assay); GOPC-ROS1 (Cell-free assay); ALK (Cell-free assay); ALK variants (Cell-free assay) <1 nM; <1 nM; <1 nM; <4 nM; <4 nMIn vitroEnsartinib potently inhibits both wild-type ALK and all evaluated ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM. Besides ALK, ensartinib also potently inhibits TPM3-TRKA, TRKC and GOPC-ROS1 with an IC50 of <1 nM, and inhibits EphA2, EphA1, EphB1 and c-MET with an IC50 of 1-10 nM. Specification: 10mM in DMSO Molecular Formula: C26H29Cl4FN6O3 Molecular Weight: 634.36 PubChem CID: 138320013 Isomeric SMILES: C[C@@H]1CN(C[C@@H](N1)C)C(=O)C2=CC=C(C=C2)NC(=O)C3=NN=C(C(=C3)O[C@H](C)C4=C(C=CC(=C4Cl)F)Cl)N.Cl.Cl