AZ-23
AZ-23 Basic information
- Product Name:
- AZ-23
- Synonyms:
-
- (S)-5-chloro-N2-(1-(5-fluoropyridin-2-yl)ethyl)-N4-(5-isopropoxy-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
- AZ-23
- 5-Chloro-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-N'-(5-isopropoxy-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
- AZ23; AZ-23
- 2,4-Pyrimidinediamine, 5-chloro-N2-[(1S)-1-(5-fluoro-2-pyridinyl)ethyl]-N4-[5-(1-methylethoxy)-1H-pyrazol-3-yl]-
- Tropomyosin related kinase receptor,Inhibitor,inhibit,AZ-23,Trk Receptor
- AZ-23, 10 mM in DMSO
- CAS:
- 915720-21-7
- MF:
- C17H19ClFN7O
- MW:
- 391.8304632
- Mol File:
- 915720-21-7.mol
AZ-23 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
AZ-23 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 ) |
IC 50
TrkA: 2 nM (IC50); TrkB: 8 nM (IC50)
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