Repotrectinib is a potent ROS1 and TRK Inhibitor
Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits ALK G1202R with an IC50 of 1.26 nM. Besides, it inhibits ALK L1196M with an IC50 of 1.08 nM)....
Crizotinib is an Orally Active, ATP-Competitive ALK and c-Met inhibitor
In this article, we will introduce an orally bioavailable, ATP-competitive ALK and c-Met inhibitor, Crizotinib. The IC50 values for ALK and c-Met kinases are 20 and 8 nM, respectively. Additionally, in cell-based assays, Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM, respectively. In...