AZ-23是ATP-竞争型，有口服活性的Trk激酶A/B/C抑制剂，IC50值分别为2nM(TrkA)，8nM(TrkB)，24nM(FGFR1)，52nM(Flt3)，55nM(Ret)，84nM(MuSk)，99nM(Lck)。
CAS：915720-21-7
分子式：C17H19ClFN7O
分子量：391.83
纯度：98%
存储：Store at -20°C

Background:

AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.

AZ-23 potently and selectivity inhibits Trk phosphorylation in cells. AZ-23 potently inhibits Trk-mediated survival (EC50 of 2 nM). AZ-23 Inhibits Trk-Dependent Survival in MCF10ATrkA-δ and TF-1 Cell Lines[1].

AZ-23 shows in vivo TrkA kinase inhibition and efficacy in mice following oral administration in a TrkA-driven allograft model and significant tumor growth inhibition in a Trk-expressing xenograft model of neuroblastoma[1].

[1]. Thress K, et al. Identification and preclinical characterization of AZ-23, a novel, selective, and orally bioavailable inhibitor of the Trk kinase pathway. Mol Cancer Ther. 2009 Jul; 8(7):1818-27.