Art. -Nr.: HY-15590

AZ-23

(Synonyms: AZD1332)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

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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Reinheit: 98.92%
CAS. Nr.: 915720-21-7
Formel: C₁₇H₁₉ClFN₇O
Molecular Weight:391.83

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZ-23 Chemical Structure

CAS. Nr.: 915720-21-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

TrkA

2 nM (IC₅₀)

TrkB

8 nM (IC₅₀)

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.02 μM Compound: AZ-23	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.059 μM Compound: AZ-23	Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.13 μM Compound: AZ-23	Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
KM12	IC₅₀	0.021 μM Compound: AZ-23	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
MCF-10A	IC₅₀	1.51 nM Compound: 1a, AZ-23	Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA	[PMID: 24900538]
MCF-10A	IC₅₀	2430 nM Compound: 1a, AZ-23	Cytotoxicity against human MCF10A cells Cytotoxicity against human MCF10A cells	[PMID: 24900538]
RD	IC₅₀	5.3 μM Compound: 8, AZ-23, NCGC00250381	Antiproliferative activity against human RD cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human RD cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 23787099]
Sf9	IC₅₀	2.81 nM Compound: T1; AZ-23	Inhibition of TRKA E735A mutant (unknown origin) expressed in baculovirus infected sf9 cells assessed as kinase domain dimerization by HTRF assay Inhibition of TRKA E735A mutant (unknown origin) expressed in baculovirus infected sf9 cells assessed as kinase domain dimerization by HTRF assay	[PMID: 31699609]
SJRH30	IC₅₀	1.8 μM Compound: 8, AZ-23, NCGC00250381	Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 23787099]

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].

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

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].

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

Chemical Information

CAS. Nr. 915720-21-7
Appearance Solid
Molecular Weight 391.83
Formel C₁₇H₁₉ClFN₇O
Color White to off-white
SMILES

CC(OC1=CC(NC2=NC(N[C@H](C3=NC=C(F)C=C3)C)=NC=C2Cl)=NN1)C
Synonyms

AZD1332
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Mol Cell Proteomics

Phosphoproteome Profiling of the Receptor Tyrosine Kinase MuSK Identifies Tyrosine Phosphorylation of Rab GTPases. [Abstract]

2022 Apr;21(4):100221. PMID: 35227894

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (319.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Thress K, et al. Identification and preclinical characterization of AZ-23, a novel, selective, and orally bioavailable inhibitor of the Trk kinase pathway. Mol Cancer Ther. 2009 Jul; 8(7):1818-27. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5521 mL	12.7606 mL	25.5213 mL	63.8032 mL
	5 mM	0.5104 mL	2.5521 mL	5.1043 mL	12.7606 mL
	10 mM	0.2552 mL	1.2761 mL	2.5521 mL	6.3803 mL
	15 mM	0.1701 mL	0.8507 mL	1.7014 mL	4.2535 mL
	20 mM	0.1276 mL	0.6380 mL	1.2761 mL	3.1902 mL
	25 mM	0.1021 mL	0.5104 mL	1.0209 mL	2.5521 mL
	30 mM	0.0851 mL	0.4254 mL	0.8507 mL	2.1268 mL
	40 mM	0.0638 mL	0.3190 mL	0.6380 mL	1.5951 mL
	50 mM	0.0510 mL	0.2552 mL	0.5104 mL	1.2761 mL
	60 mM	0.0425 mL	0.2127 mL	0.4254 mL	1.0634 mL
	80 mM	0.0319 mL	0.1595 mL	0.3190 mL	0.7975 mL
	100 mM	0.0255 mL	0.1276 mL	0.2552 mL	0.6380 mL

Keywords

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AZ-23

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Chemical Probe Library

Targeted Diversity Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ-23

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ-23

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Chemical Probe Library

Targeted Diversity Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ-23

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ-23 Related Classifications

Art. -Nr.: HY-15590