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Antiviral API
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AZ-960
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| Category | Virus Protease |
| CAS | 905586-69-8 |
| Description | AZ-960 is an ATP-competitive inhibitor of JAK2 with Ki value of 0.45 nM. It inhibits proliferation in a SET-2 human megakaryoblastic cell line harboring the JAK2V617F mutation with GI50 value of 33 nM. |
Product Information
| Synonyms | (S)-5-Fluoro-2-((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)-; 5-Fluoro-2-{[(1S)-1-(4-fluorophenyl)ethyl]amino}-6-[(5-methyl-1H-pyrazol-3-yl)amino]nicotinonitrile |
| IUPAC Name | 5-fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile |
| Molecular Weight | 354.36 |
| Molecular Formula | C18H16F2N6 |
| Canonical SMILES | CC1=CC(=NN1)NC2=C(C=C(C(=N2)NC(C)C3=CC=C(C=C3)F)C#N)F |
| InChI | InChI=1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1 |
| InChIKey | SUNXHXDJOIXABJ-NSHDSACASA-N |
| Boiling Point | 515.2±50.0°C (Predicted) |
| Flash Point | 265.4±30.1 °C |
| Purity | >98% |
| Density | 1.37±0.1 g/cm3 (Predicted) |
| Solubility | Soluble in DMSO |
| Appearance | Light Yellow to Yellow Solid |
| Storage | Store at 2-8°C |
| Complexity | 503 |
| Exact Mass | 354.14045086 |
| Index Of Refraction | 1.628 |
| In Vitro | AZ 960 inhibits JAK2 enzyme activity with 0.45 nM for Ki and IC50<3 nM. In addition, 0.1 μM AZ960 also inhibits 31 of 83 kinases, such as JAK3 (IC50 of 9 nM), TrkA, Aurora, and ARK5. AZ 960 acts on TEL-JAK2 cells and inhibits STAT5 phosphorylation with an average IC50 of 15 nM. AZ 960 effectively inhibits TEL-JAK2, -JAK1, -JAK3, and -Tyk2 cell proliferation with GI50 25 nM, 230 nM, 279 nM, and 214 nM, respectively. Moreover, AZ 960 also effectively inhibits SET-2 cell proliferation with an average GI50 of 33 nM. AZ 960 causes growth arrest and Apoptosis in human T-cell lymphophilophilic virus type 1 (HTLV-1) infected T cells (MT-1 and MT-2), and inhibits Bcl-xL by enhancing the antiproliferative effect of AZ 960 on MT-1 cells by small interference RNA. Recent studies have shown that AZ 960 significantly inhibits clonal growth of newly isolated AML cells in patients and induces Apoptosis. |
| PSA | 95.88000 |
| Target | JAK; Apoptosis; Parasite; Virus Protease |
| Vapor Pressure | 0.0±1.3 mmHg at 25°C |
| XLogP3-AA | 4.4 |
