There are more well-characterized tools, in particular Laratrectinib which is both approved for human use and better profiled for selectivity against more kinases (link)or perhaps clinical compounds AZD7451.
Cell Concentration notes: Fig1 of the 2nd reference shows a plateau of activity from 50-500 nM in GOT1 cell.
Ref1 demonstrates sufficient IV and PO exposure for human tumor xenograft studies plus demonstrated efficacy. However, given the ~86% similarity between human and rat/mouse TRKA, I would recommend confirming rat or mouse potency comparable to humans before using rats or mice as an efficacy model in a non-human xenograft study
4 Aug 2021 )