AZ 960

Modify Date: 2024-01-02 19:42:17

AZ 960 Structure
AZ 960 structure
Common Name AZ 960
CAS Number 905586-69-8 Molecular Weight 354.357
Density 1.4±0.1 g/cm3 Boiling Point 515.2±50.0 °C at 760 mmHg
Molecular Formula C18H16F2N6 Melting Point N/A
MSDS N/A Flash Point 265.4±30.1 °C

 Use of AZ 960


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

 Names

Name 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile
Synonym More Synonyms

 AZ 960 Biological Activity

Description AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
Related Catalog
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].
Cell Assay 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].
References

[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.

[2]. 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.

[3]. 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.

[4]. 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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 515.2±50.0 °C at 760 mmHg
Molecular Formula C18H16F2N6
Molecular Weight 354.357
Flash Point 265.4±30.1 °C
Exact Mass 354.140442
PSA 95.88000
LogP 6.09
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.628
Storage condition -20℃

 Synonyms

AZ 960,AZ960
AZ 960
S2214_Selleck
UNII-M63IS9PTJF
5-Fluoro-2-{[(1S)-1-(4-fluorophenyl)ethyl]amino}-6-[(5-methyl-1H-pyrazol-3-yl)amino]nicotinonitrile
3-Pyridinecarbonitrile, 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-
cc-210
AZ960