Art. -Nr.: HY-10411

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AZ960

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AZ960 is a potent and specific inhibitor of the JAK2 kinase with a K_i of 0.45 nM.

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Reinheit: 97.08%
CAS. Nr.: 905586-69-8
Formel: C₁₈H₁₆F₂N₆
Molecular Weight:354.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AZ960 Chemical Structure

CAS. Nr.: 905586-69-8

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AZ960 is a potent and specific inhibitor of the JAK2 kinase with a K_i of 0.45 nM.

IC₅₀ & Target^[4]

JAK2

0.45 nM (Ki)

JAK2

<3 nM (IC₅₀)

JAK3

9 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	0.024 μM Compound: 1c, AZ960	Inhibition of TEL-fused JAK2-induced proliferation of mouse BA/F3 cells Inhibition of TEL-fused JAK2-induced proliferation of mouse BA/F3 cells	[PMID: 21493067]
BaF3	GI₅₀	0.35 μM Compound: 1c, AZ960	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	[PMID: 21493067]
INS1	IC₅₀	10 μM Compound: AZ960	Cytotoxicity against rat INS-1 cells assessed as cell growth inhibition Cytotoxicity against rat INS-1 cells assessed as cell growth inhibition	[PMID: 27519462]
SET-2	GI₅₀	0.033 μM Compound: 1c, AZ960	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	[PMID: 21493067]

In Vitro

AZ960 inhibits Jak2 kinase with a K_i 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 K_i 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

CAS. Nr. 905586-69-8
Appearance Solid
Molecular Weight 354.36
Formel C₁₈H₁₆F₂N₆
Color Light yellow to yellow
SMILES

N#CC1=CC(F)=C(NC2=NNC(C)=C2)N=C1N[C@H](C3=CC=C(F)C=C3)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

In Vitro:

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.

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

2.8220 mL

14.1099 mL

28.2199 mL

5 mM

0.5644 mL

2.8220 mL

5.6440 mL

10 mM

0.2822 mL

1.4110 mL

2.8220 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, 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.

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: ≥ 2.5 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
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]. 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]

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, 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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AZ960

Anti-Infection Compound Library

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ960

Alle JAK Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ960 Related Classifications

HY-10411 Related Classifications