. 2020 Aug 20;23(8):719–729. [Article in Chinese] doi: 10.3779/j.issn.1009-3419.2020.102.34

1.

恩沙替尼及同类药的作用靶点

Targets of ensatinib and similar drugs

ALK-TKI	Targets	IC₅₀ or Ki ^* (nmol/L)	Ref.
ALK-TKI: anaplastic lymphoma kinase-tyrosine kinase inhibitor; IC₅₀: 50% inhibitory concentration; EGFR: epidermal growth factor receptor; ^Ki and IC₅₀ values by in vitro* enzymatic studies.
Ensartinib	ALK ROS1 MET AXL	1.7 19 1.8 35	[9]
Crizotinib	ALK ROS1 MET	0.69^* N.D. 4^*	[10, 11]
Ceritinib	ALK IGF-1R INSR STK22D	0.15 8 7 23	[12-14]
Alectinib	ALK RET	1.9 4.8	[15, 16]
Brigatinib	ALK ROS1 FLT3 EGFR L858R	0.6 1.9 2.1 1.5	[17, 18]
Lorlatinib	ALK ROS1	1.3 < 0.02^*	[19]