| Identification | Back Directory | [Name]
AZ-23 | [CAS]
915720-21-7 | [Synonyms]
AZ-23
AZ23; AZ-23
5-Chloro-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-N'-(5-isopropoxy-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
(S)-5-chloro-N2-(1-(5-fluoropyridin-2-yl)ethyl)-N4-(5-isopropoxy-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
2,4-Pyrimidinediamine, 5-chloro-N2-[(1S)-1-(5-fluoro-2-pyridinyl)ethyl]-N4-[5-(1-methylethoxy)-1H-pyrazol-3-yl]- | [Molecular Formula]
C17H19ClFN7O | [MDL Number]
MFCD17215208 | [MOL File]
915720-21-7.mol | [Molecular Weight]
391.83 |
| Hazard Information | Back Directory | [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 ) | |
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NCE Biomedical Co.,Ltd.
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SPIRO PHARMA
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www.spiropharma.com.cn |
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