1. Epigenetics
    Stem Cell/Wnt
    Anti-infection
    JAK/STAT Signaling
    Apoptosis
  2. JAK
    Parasite
    Apoptosis
    Virus Protease
  3. AZ960

AZ960 

Cat. No.: HY-10411 Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

AZ960 Chemical Structure

AZ960 Chemical Structure

CAS No. : 905586-69-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 117 In-stock
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
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Description

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

IC50 & Target

JAK2

0.45 nM (Ki)

JAK2

<3 nM (IC50)

JAK3

9 nM (IC50)

In Vitro

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].

Molecular Weight

354.36

Formula

C₁₈H₁₆F₂N₆

CAS No.

905586-69-8

SMILES

N#CC1=CC(F)=C(NC2=NNC(C)=C2)N=C1N[[email protected]](C3=CC=C(F)C=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (84.66 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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].

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

References
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Keywords:

AZ960AZ 960AZ-960JAKParasiteApoptosisVirus ProteaseJanus kinaseInhibitorinhibitorinhibit

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Product name:
AZ960
Cat. No.:
HY-10411
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