915720-21-7
915720-21-7 structure
- Name: AZ-23
- Chemical Name: 5-chloro-2-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine
- CAS Number: 915720-21-7
- Molecular Formula: C17H19ClFN7O
- Molecular Weight: 391.831
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Trk Receptor
- Create Date: 2016-09-17 11:54:20
- Modify Date: 2024-01-11 11:32:57
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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.
| Name | 5-chloro-2-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine |
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| Synonyms |
5-Chloro-N-[(1S)-1-(5-fluoro-2-pyridinyl)ethyl]-N-(3-isopropoxy-1H-pyrazol-5-yl)-2,4-pyrimidinediamine
az-23 2,4-Pyrimidinediamine, 5-chloro-N-[(1S)-1-(5-fluoro-2-pyridinyl)ethyl]-N-[3-(1-methylethoxy)-1H-pyrazol-5-yl]- unii-009omi967n |
| Description | 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. |
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| Related Catalog | |
| Target |
TrkA:2 nM (IC50) TrkB:8 nM (IC50) |
| In Vitro | 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]. |
| 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[1]. |
| Cell Assay | Exponentially growing TF-1 cells are treated with various concentrations of AZ-23 and then incubated for an additional 72 h at 37°C in either growth or basal medium plus 100 ng/mL NGF. Cell proliferation is measured using MTS solution[1]. |
| Animal Admin | Mice[1] Tumor-bearing mice are given a single, oral dose of compound and individual mice are sacrificed at various time points postdose (2, 6, 16, or 24 hours). Tumors are excised and homogenized and the resulting tumor lysates are analyzed using an ELISA for pTrkA[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 596.1±60.0 °C at 760 mmHg |
| Molecular Formula | C17H19ClFN7O |
| Molecular Weight | 391.831 |
| Flash Point | 314.3±32.9 °C |
| Exact Mass | 391.132355 |
| PSA | 103.87000 |
| LogP | 2.64 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.655 |