TPX-0005

TPX-0005 is a potent ALK inhibitor. It inhibits WT ALK (IC50 1.01 nM) and mutant ALKs including ALK G1202R (IC₅₀ = 1.26 nM) and ALK L1196M (IC₅₀ = 1.08 nM). Moreover, TPX-0005 effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts. TPX-0005 is also a potent SRC inhibitor (IC₅₀ = 5.3 nM).