1. Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. AZ-23

AZ-23 (Synonyms: AZ23; AZ 23)

Cat. No.: HY-15590 Purity: 99.93%
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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 560 In-stock
Estimated Time of Arrival: December 31
50 mg USD 960 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (319.02 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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AZ-23
Cat. No.:
HY-15590
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