AZ-23
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.92%
- CAS 番号: 915720-21-7
- 分子式: C17H19ClFN7O
- 分子量:391.83
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Kinase Inhibitor Library
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MedChemExpress（MCE）の使用を引用している文献 AZ-23
More
生物活性
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TrkA 2 nM (IC50) |
TrkB 8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.02 μM
Compound: AZ-23
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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
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[PMID: 35617855] |
| BaF3 | IC50 |
0.059 μM
Compound: AZ-23
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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
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[PMID: 35617855] |
| BaF3 | IC50 |
0.13 μM
Compound: AZ-23
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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
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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
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[PMID: 35617855] |
| MCF-10A | IC50 |
1.51 nM
Compound: 1a, AZ-23
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Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA
Cytotoxicity against human MCF10A cells overexpressing constitutively active TRKA
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[PMID: 24900538] |
| MCF-10A | IC50 |
2430 nM
Compound: 1a, AZ-23
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Cytotoxicity against human MCF10A cells
Cytotoxicity against human MCF10A cells
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[PMID: 24900538] |
| RD | IC50 |
5.3 μM
Compound: 8, AZ-23, NCGC00250381
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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
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[PMID: 23787099] |
| Sf9 | IC50 |
2.81 nM
Compound: T1; AZ-23
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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
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[PMID: 31699609] |
| SJRH30 | IC50 |
1.8 μM
Compound: 8, AZ-23, NCGC00250381
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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
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[PMID: 23787099] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 915720-21-7
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性状 Solid
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分子量 391.83
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分子式 C17H19ClFN7O
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Color White to off-white
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SMILES
CC(OC1=CC(NC2=NC(N[C@H](C3=NC=C(F)C=C3)C)=NC=C2Cl)=NN1)C
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別名
AZD1332
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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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
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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.
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.
純度とドキュメンテーション
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データシート (272 KB)
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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)
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取扱説明書 (2659 KB)
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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