LOXO-195

  • Chemical Properties
CAS No. 2097002-61-2 Cat. No. BCP20662
Name LOXO-195
Synonyms LOXO 195; LOXO195;Selitrectinib;
Formula C20H21FN6O M. Wt 380.43
  • Biological Activity
Description LOXO-195 is a potent and selective TRK inhibitor capable of addressing potential mechanisms of acquired resistance that may emerge in patients receiving larotrectinib (LOXO-101) or multikinase inhibitors with anti-TRK activity. LOXO-195 demonstrated potent inhibition of TRK fusions, including critical acquired resistance mutations, in enzyme and cellular assays, with minimal activity against other kinases. In diverse TRK fusion mouse models, LOXO-195 inhibited phospho-ERK and caused dramatic tumor growth inhibition, superior to first generation TRK inhibitors, without significant toxicity.
Pathways Angiogenesis/Protein Tyrosine Kinase 
Targets Trk Receptor 

Structure

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