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Basic Info

  • Grade: Pharmaceutical Grade

    Factory Location: Zhongcheng Future Industrial Park, Hangcheng Avenue, Baoan District, Shenzhen

    Main Sales Markets: North America,Central/South America,Western Europe,Eastern Europe,Asia,Middle East,Africa

  • Contract Manufacturing: CRO,CMO

  • Sample Provided: yes

    Payment Terms: L/C

    Repotrectinib Biological Activity

    Description: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.

    Target:IC50: 5.3 nM (SRC), 1.01 nM (WT ALK), 1.26 nM (ALK G1202R), 1.08 nM (ALK L1196M)

    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.

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

     

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