Ensartinib 是一种有效的ALK抑制剂，对许多具有crizotinib抗性的ALK突变型和中枢神经系统转移具有高活性。它能有效地抑制野生型ALK和ALK变体（F1174, C1156Y, L1196M, S1206R, T1151和G1202R突变型），IC50小于4 nM。

Ensartinib (X-396) 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.

Ensartinib is a selective ALK inhibitor, and provids promising advantages in terms of both Clinicalal activity and safety[1].

1365267-27-1

C25H25Cl2FN6O3

547.41

恩沙替尼;Ensartinib;X-396

DMSO:37 mg/mL (67.59 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years