CAS 905586-69-8|AZ 960
Introduction：Basic information about CAS 905586-69-8|AZ 960, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| 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 | / |
| MSDS | / | Flash Point | 265.4±30.1 °C |
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 BiologicalActivity
| 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. |
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 |
| InChIKey | SUNXHXDJOIXABJ-NSHDSACASA-N |
| SMILES | Cc1cc(Nc2nc(NC(C)c3ccc(F)cc3)c(C#N)cc2F)n[nH]1 |
| 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 |
