Catalog No.: PC-73061Not For Human Use, Lab Use Only.
DS-6051b (Taletrectinib, DS 6051b) is a new-generation selective ROS1/NTRK inhibitor, potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in ATP-competitive manner (IC50=1-10 nM).
DS-6051b (Taletrectinib, DS 6051b) is a new-generation selective ROS1/NTRK inhibitor, potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in ATP-competitive manner (IC50=1-10 nM).
DS-6051b completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but not other 152 kinases.
DS-6051b inhibits the growth of the CD74-ROS1 overexpressed Ba/F3 cells and the ROS1 fusion-positive HCC78 cancer cell line with a lower IC50 than crizotinib.
DS-6051b shows activity against NTRK1-TKI-resistant mutants including G595R (IC50<100 nM), effectively inhibits crizotinib-resistant ROS1 secondary mutations, including G2032R.
DS-6051b demonstrates efficacy in ROS1- or NTRK-rearranged cancer in preclinical models, including crizotinib-resistant ROS1 positive cancer with secondary kinase domain mutations especially G2032R mutation.
