alk/ros1-in-1

ALK/ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK/ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme).

PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).

Entrectinib-d4 是 Paquinimod 的氘代标记同位素。Entrectinib 是一种口服有效的 TrkA/B/C、ROS1 和 ALK 抑制剂，能够穿透血脑屏障并具有中枢神经系统活性，其 IC50 值分别为 1 nM、3 nM、5 nM、12 nM 和 7 nM。它可以诱导癌细胞凋亡和阻止细胞周期，展现出强劲的抗肿瘤活性，还能减轻博来霉素引起的小鼠肺纤维化。

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) 是一种氘代形式的Entrectinib。Entrectinib (NMS-E628) 是一种有效的口服制剂，能够透过血脑屏障并作用于中枢神经系统，作为TrkA/B/C、ROS1和ALK的抑制剂，其IC50值分别为1, 3, 5, 12和7 nM。Entrectinib 可以诱导癌细胞凋亡和细胞周期停滞，展现良好的抗肿瘤活性，并能减轻由博来霉素引起的小鼠肺纤维化。