AZ-23

Product NameAZ-23
CAS915720-21-7
MFC17H19ClFN7O
MW391.8304632
EINECS
MOL File915720-21-7.mol

Chemical Properties

Boiling point	596.1±60.0 °C(Predicted)
Density	1.411
storage temp.	Store at -20°C
solubility	DMSO:125.0(Max Conc. mg/mL);319.02(Max Conc. mM)
pka	12.37±0.10(Predicted)
form	Solid
color	White to off-white

Usage And Synthesis

Uses

5-Chloro-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-N'-(5-isopropoxy-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZ-23) is a potent and selective tyrosine kinase inhibitor which may be used in the therapeutic treatment of cancers.

Biological Activity

AZ-23 is an ATP-competitive, orally active Trk kinase A/B/C inhibitor with IC50 values of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3) , 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck).

in vitro

AZ-23 potently and selectivity inhibits Trk phosphorylation in cells. AZ-23 potently inhibits Trk-mediated survival (EC ₅₀ of 2 nM). AZ-23 Inhibits Trk-Dependent Survival in MCF10ATrkA-Δ and TF-1 Cell Lines.

in vivo

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 .

target

TrkA

2 nM (IC ₅₀ )

TrkB

8 nM (IC ₅₀ )