alk/ros1 in 1

ALK/ROS1 inhibitor 2e HCL possesses anti-apoptotic, anti-proliferative and anti-tumour activities.

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 is the deuterium-labeled isotope of Paquinimod. Entrectinib is an orally active inhibitor of TrkA/B/C, ROS1, and ALK, capable of crossing the blood-brain barrier and possessing central nervous system activity, with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. It induces apoptosis and cell cycle arrest in cancer cells, exhibits antitumor efficacy, and mitigates bleomycin-induced pulmonary fibrosis in mice.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is the deuterated form of Entrectinib. Entrectinib (NMS-E628) is an orally bioavailable inhibitor that effectively crosses the blood-brain barrier and exhibits central nervous system activity. It targets TrkA/B/C, ROS1, and ALK with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. Entrectinib induces apoptosis and cell cycle arrest in cancer cells, demonstrates antitumor properties, and alleviates bleomycin-induced pulmonary fibrosis in mice.