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

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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AZ-23

AZ-23 構造式

CAS 番号 : 915720-21-7

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 176 在庫あり
Solution
10 mM * 1 mL in DMSO USD 176 在庫あり
Solid
5 mg $160 在庫あり
10 mg $260 在庫あり
25 mg $560 在庫あり
50 mg $960 在庫あり
100 mg $1650 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

Trk Receptor アイソフォーム固有の製品をすべて表示:

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  • プロトコル

  • 純度とドキュメンテーション

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
0.02 3
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
0.02 3
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
0.02 3
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 3
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
0.059 3
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
0.059 3
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 3
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]
BaF3 IC50
0.13 3
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]
BaF3 IC50
0.13 3
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 3
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 1
Compound: 1a, AZ-23
Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA
Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA
[PMID: 24900538]
RD IC50
5.3 3
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 1
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]
KM12 IC50
0.021 3
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]
Sf9 IC50
2.81 1
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]
KM12 IC50
0.021 3
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 1
Compound: 1a, AZ-23
Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA
Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA
[PMID: 24900538]
SJRH30 IC50
1.8 3
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]
RD IC50
5.3 3
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]
MCF-10A IC50
2430 1
Compound: 1a, AZ-23
Cytotoxicity against human MCF10A cells
Cytotoxicity against human MCF10A cells
[PMID: 24900538]
SJRH30 IC50
1.8 3
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]
RD IC50
5.3 3
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]
MCF-10A IC50
2430 1
Compound: 1a, AZ-23
Cytotoxicity against human MCF10A cells
Cytotoxicity against human MCF10A cells
[PMID: 24900538]
SJRH30 IC50
1.8 3
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]
Sf9 IC50
2.81 1
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]
体外実験

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.

体内実験

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.

分子量

391.83

分子式

C17H19ClFN7O

CAS 番号
Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

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体積 (開始)

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体内:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献
細胞実験
[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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

Complete Stock Solution Preparation Table

* 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.

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
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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Inquiry Information

製品名:
AZ-23
製品番号:
HY-15590
数量:
MCE 日本正規代理店: