Lorlatinib (PF-06463922) 是一种选择性、口服活性、可穿透大脑、ATP 竞争性 ROS1/ALK 抑制剂，具有抗癌活性，对 ROS1、野生型 ALK 和 ALKL1196M 的 Ki 值分别为 <0.025 nM、<0.07 nM 和 0.7 nM。Lorlatinib 靶向 EML4-ALK 并抑制 ALK 磷酸化，对 ALKL1196、ALKG1269A、ALK1151Tins 和 ALKG1202R 的 IC50 分别为 15-43 nM、14-80 nM、38-50 nM 和 77-113 nM。

Entrectinib（NMS-E628）是一种口服有效的、可穿透血脑屏障的TrkA/B/C、ROS1和ALK抑制剂，对它们的IC50值分别为1、3、5、12和7 nM。它在癌细胞中诱导凋亡和细胞周期停滞，显示出抗肿瘤活性，并减轻小鼠中博来霉素引起的肺纤维化。

TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.

LY2801653 2HCl is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase (Ki= 2 nM).

Crizotinib HCl is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM, respectivley.

Taletrectinib is a new-generation selective ROS1/Trk Receptor inhibitor with IC50 values of 0.207nM, 0.622nM, 2.28nM and 0.98nM for ROS1, Trk Receptor A, B and C, respectively. It induces dramatic growth inhibition of both wild type and G2032R mutant ROS1-rearranged cancers or NTRK-rearranged cancers in vitro and in vivo.