AZ-23 is an inhibitor of ATP-competitive and Trk kinase A/B/C. For TrkA, TrkB, FGFR1, Flt3, Ret, MuSk, Lck, the IC50s values are 2 nM, 8 nM, 24 nM, 52 nM, 55 nM, 84 nM, 99 nM, respectively.

TrkB:8 nM, TrkA:2 nM

AZ-23 selectively and potently inhibits Trk phosphorylation in cells, with an EC50 of 2 nM for Trk-mediated survival. It also inhibits Trk-dependent survival in MCF10ATrkA-Δ and TF-1 cell lines[1].

Following oral administration in a TrkA-driven allograft model, AZ-23 demonstrates effective in vivo inhibition of TrkA kinase and efficacy in mice. It also significantly inhibits tumor growth in a Trk-expressing xenograft model of neuroblastoma[1].