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.

PF-06463922 is an orally available, CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with Ki of < 0.02 nM, < 0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.

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.

Entrectinib is an oral pan-Trk, ROS1, and ALK inhibitor, with IC50 of 1.7/0.1/0.1 nM, 0.2 nM, and 1.6 nM for Trk A/B/C, ROS1, and ALK, 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.