905586-69-8
905586-69-8 structure
- Name: AZ 960
- Chemical Name: 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile
- CAS Number: 905586-69-8
- Molecular Formula: C18H16F2N6
- Molecular Weight: 354.357
- Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Ethylpyridine
- Create Date: 2016-08-29 10:29:05
- Modify Date: 2025-08-25 17:09:17
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AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
| Name | 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile |
|---|---|
| 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 |
| 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 |
| 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℃ |