Repotrectinib

  • Chemical Properties
CAS No. 1802220-02-5 Cat. No. BCP19778
Name Repotrectinib
Synonyms TPX-0005;TPX 0005; TPX0005;
Formula C18H18FN5O2 M. Wt 355.37
  • Biological Activity
Description 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.TPX-0005 is a Src/FAK/Janus kinase 2 (JAK2) inhibitor. TPX-0005 plus EGFR TKI suppressed expression and activation of RTKs and downstream signaling intermediates. Co-expression of CDCP1 and AXL is often observed in EGFR-mutation-positive tumors, limiting the efficacy of EGFR TKIs. Co-treatment with EGFR TKI and TPX-0005 warrants testing.
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway Wnt/Stem Cell Epigenetics 
Targets Trk Receptor Src/Bcr Abl JAK FAK ALK 

Structure

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