1. Protein Tyrosine Kinase/RTK
  2. Trk Receptor

AZ-23 (Synonyms: AZ23; AZ 23)

Cat. No.: HY-15590
Handling Instructions

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.

For research use only. We do not sell to patients.

AZ-23 Chemical Structure

AZ-23 Chemical Structure

CAS No. : 915720-21-7

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1]

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5521 mL 12.7606 mL 25.5213 mL
5 mM 0.5104 mL 2.5521 mL 5.1043 mL
10 mM 0.2552 mL 1.2761 mL 2.5521 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

391.83

Formula

C₁₇H₁₉ClFN₇O

CAS No.

915720-21-7

SMILES

CC(OC1=CC(NC2=NC(N[[email protected]](C3=NC=C(F)C=C3)C)=NC=C2Cl)=NN1)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AZ-23
Cat. No.:
HY-15590
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AZ-23

Cat. No.: HY-15590