AZ960
Based on 1 publication(s) in Google Scholar
AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
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- Pureza: 97.08%
- No. CAS: 905586-69-8
- Fòrmula: C18H16F2N6
- Peso molecular:354.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) AZ960
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Actividad biológica
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JAK2 0.45 nM (Ki) |
JAK2 <3 nM (IC50) |
JAK3 9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | GI50 |
0.024 μM
Compound: 1c, AZ960
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Inhibition of TEL-fused JAK2-induced proliferation of mouse BA/F3 cells
Inhibition of TEL-fused JAK2-induced proliferation of mouse BA/F3 cells
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[PMID: 21493067] |
| BaF3 | GI50 |
0.35 μM
Compound: 1c, AZ960
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Inhibition of TEL-fused JAK3-induced proliferative activity against mouse BA/F3 cells
Inhibition of TEL-fused JAK3-induced proliferative activity against mouse BA/F3 cells
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[PMID: 21493067] |
| INS1 | IC50 |
10 μM
Compound: AZ960
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Cytotoxicity against rat INS-1 cells assessed as cell growth inhibition
Cytotoxicity against rat INS-1 cells assessed as cell growth inhibition
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[PMID: 27519462] |
| SET-2 | GI50 |
0.033 μM
Compound: 1c, AZ960
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Growth inhibition of human SET2 cells expressing JAK2 V617F mutant after 48 hrs by alamar blue assay
Growth inhibition of human SET2 cells expressing JAK2 V617F mutant after 48 hrs by alamar blue assay
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[PMID: 21493067] |
AZ960 inhibits Jak2 kinase with a Ki of 0.45 nM. Z960 possesses much less potent activity against Jak1, 3, and TYK2. AZ960 is active against other kinases, including TrkA, Aurora-A, and FAK, with IC50 of around 0.1 μM. AZ960 effectively induces growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1–infected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of Jak2 and Bcl-2 family proteins including Bcl-2 and Mcl-1[2].
AZ960 potently inhibits the clonogenic growth and induces apoptosis of freshly isolated acute myelogenous leukemia cells from patients in association with cleavage of caspase 3 and down regulation of anti-apoptotic Bcl-xL proteins[1].
AZ960 has a Ki of 1.25 μM for T. brucei extracellular signal-regulated kinase 8 (TbERK8). It inhibits TbERK8 with an IC50 of 120 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 905586-69-8
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Appearance Solid
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Peso molecular 354.36
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Fòrmula C18H16F2N6
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Color Light yellow to yellow
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SMILES
N#CC1=CC(F)=C(NC2=NNC(C)=C2)N=C1N[C@H](C3=CC=C(F)C=C3)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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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
Solvente y solubilidad
DMSO : ≥ 30 mg/mL (84.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (7.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protocolo
AZ960 is dissolved in 100% DMSO to a 0.01 M. HTLV-1–infected T cells and MOLT-4 cells are cultured with various concentrations of AZ960 (0.03-1 μM) for 2 days in 96-well plates. Peripheral blood lymphocytes are activated by phytohemagglutinin (PHA; 5 ng/mL) for 1 hour, then cultured with various concentrations of AZ960 (0.03–1 μM) for 2 days in 96-well plates. After culture, cell number and viability are evaluated by measuring the mitochondrial-dependent conversion of the MTT to a colored formazan product[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ikezoe T, et al. Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia. Int J Cancer. 2011 Nov 15;129(10):2512-21. [Content Brief]
[2]. Gozgit JM, et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43. [Content Brief]
[3]. Yang J, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95. [Content Brief]
[4]. Valenciano AL, et al. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. Bioorg Med Chem. 2016 Oct 1;24(19):4647-51. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8220 mL | 14.1099 mL | 28.2199 mL | 70.5497 mL |
| 5 mM | 0.5644 mL | 2.8220 mL | 5.6440 mL | 14.1099 mL | |
| 10 mM | 0.2822 mL | 1.4110 mL | 2.8220 mL | 7.0550 mL | |
| 15 mM | 0.1881 mL | 0.9407 mL | 1.8813 mL | 4.7033 mL | |
| 20 mM | 0.1411 mL | 0.7055 mL | 1.4110 mL | 3.5275 mL | |
| 25 mM | 0.1129 mL | 0.5644 mL | 1.1288 mL | 2.8220 mL | |
| 30 mM | 0.0941 mL | 0.4703 mL | 0.9407 mL | 2.3517 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7055 mL | 1.7637 mL | |
| 50 mM | 0.0564 mL | 0.2822 mL | 0.5644 mL | 1.4110 mL | |
| 60 mM | 0.0470 mL | 0.2352 mL | 0.4703 mL | 1.1758 mL | |
| 80 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8819 mL |
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