AZ960

SKU: orb1300881

Description

AZ960 is a potent and selective ATP-competitive inhibitor of JAK2, demonstrating high inhibitory activity with an IC50 of less than 3 nM and a Ki of 0.45 nM. It is a valuable research tool for studying JAK-STAT signaling in hematological malignancies and myeloproliferative disorders, with utility in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 905586-69-8
• MW: 354.36
• Purity: 99.88% (May vary between batches)
• Formula: C₁₈H₁₆F₂N₆
• SMILES: C[C@H](Nc1nc(Nc2cc(C)[nH]n2)c(F)cc1C#N)c1ccc(F)cc1
• Target: Virus Protease,JAK,Parasite,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:55 mg/mL (155.21 mM);Ethanol:3 mg/mL (8.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.64 mM)

Bioactivity

• Target IC50:
  JAK3:9 nM|JAK2:0.45 nM(Ki)|JAK2:<3 nM
• In Vivo:
  AZ960 (0.1 μM) also inhibited 31 of 83 kinases, such as JAK3 (IC50: 9 nM), Aurora, TrkA, and ARK5. AZ 960 significantly inhibited the proliferation of TEL-JAK2, -JAK1, -JAK3, and -Tyk2 cells (GI50: 25/230/279/214 nM). 960 also reduced the level of STAT3/5 phosphorylation, thereby effectively inhibiting SET-2 cell proliferation (GI50: ~33 nM).AZ 960 inhibited STAT5 phosphorylation in TEL-JAK2 cells (IC50: 15 nM), and was much more effective on TEL-JAK2-driven STAT5 phosphorylation than on other JAK kinase family members (TEL-JAK1, -JAK3 and -Tyk2). -JAK3, and -TYK2)-driven cell lines.AZ 960 also caused growth arrest and apoptosis of human T-cell lymphotropic lymphotropic virus type 1-infected T-cells and inhibited Bcl-xL by potentiating the antiproliferative effect of AZ 960 on MT-1 cells via small interfering RNAs.AZ 960 significantly inhibited the clonogenic growth of newly isolated AML cells from patients AZ 960 significantly inhibited the clonal growth of newly isolated AML cells from patients and induced apoptosis.
• Cell Research:
  Cellular proliferation is evaluated using the fluorometric/colorimetric BIOSOURCE AlamarBlue Assay and read in the Spectra Max Gemini EM microplate reader. SET-2 cells are plated at 20,000 cells/well, TEL-JAK2 Ba/F3 cells at 2000 cells/well, and all other TEL-JAKs at 5000 cells/well in 96-well plates. Cells are treated with AZ 960 24 hours after plating and grown for 72 hours for SET-2 and 48 hours for TEL-JAK Ba/F3 cells. Following the indicated growth period Alamar Blue (10 μL/well) is added, cells are incubated at 37 °C in 5% CO2 for 2 hours, and fluorescence is measured at 545 (excitation) and 600 nm (emission). Data are normalized to percent of the control, and GI50 values (the concentration that causes 50% growth inhibition) are calculated using Xlfit4 version 4.2.2 for Microsoft Excel. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, AZ 960, AZ960, AZ-960, inhibit, JAK, JAK2, Janus kinase, Parasite, Inhibitor, VirusProtease, Virus Protease

Compound Identifiers

PubChem CID

25099184