ALK/ROS1-IN-1

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ROS

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1]. ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1]. ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1]. ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[1].

[1]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.