TPX-0005
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Technical Data
Description
TPX-0005 is a potent ALK/ROS1/TRK inhibitor. TPX-0005 effectively inhibited a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants. TPX-0005 potently inhibited WT ALK (IC50 1.01 nM) and mutant ALKs including ALK G1202R (1.26 nM) and ALK L1196M (1.08 nM). Moreover, TPX-0005 effectively inhibited tumor growth in vivo in ALK WT and ALK G1202R xenografts. TPX-0005 is also a potent SRC inhibitor (IC50 5.3 nM).