tcsc7628 Repotrectinib

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC₅₀ of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.

IC50 & Target: IC50: 5.3 nM (SRC), 1.01 nM (WT ALK), 1.26 nM (ALK G1202R), 1.08 nM (ALK L1196M)^[1]

In Vitro: Repotrectinib (TPX-0005) effectively overcomes this primary resistance (IC₅₀ 100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC₅₀ 13 nM) and the SRC substrate paxillin (IC₅₀ 107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib^[1].

In Vivo: Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts^[1].