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AZ 960

Names

[ CAS No. ]:
905586-69-8

[ Name ]:
AZ 960

[Synonym ]:
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

Biological Activity

[Description]:

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

[Related Catalog]:

Research Areas >> Cancer

[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.


[Related Small Molecules]

Baricitinib | Upadacitinib | Pacritinib | CYT387 | AZD1480 | Fedratinib(SAR302503,TG101348) | WP1066 | CHZ868 | AT9283 | GLPG0634 | Itacitinib | cerdulatinib | LY2784544 | SB1317 | Peficitinib

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℃

Related Compounds