NPS-1034 (NPS1034) is a potent, dual MET and AXL inhibitor with IC50 of 48 and 10.3 nM, respectively.
NPS-1034 also inhibits other kinases, such as FLT3, KIT, and DDR1.
Combined treatment with NPS-1034 and gefitinib overcomes the drug resistance caused by MET gene amplification.
Addition of NPS-1034 to gefitinib overcomes acquired resistance to gefitinib in a xenograft model.
Addition of NPS-1034 to erlotinib overcomes AXL-mediated drug resistance.
NPS-1034 treatment enhances sensitivity to EGFR-TKIs in H820 cells.
NPS-1034 inhibits ROS1 activity and cell proliferation in HCC78 cells.
