5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile;CS-184;AZ 960;(S)-5-fluoro-2-(1-(4-fluorophenyl)ethylaMino)-6-(5-Methyl-1H-pyrazol-3-ylaMino)nicotinonitrile;5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile AZ 960;(S)-5-Fluoro-2-((1-(4-fluorophenyl)ethyl)amino)-6-((5-methyl-1H-pyrazol-3-yl)amino)nicotinonit;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]-3-pyridinecarbonitrile ISO 9001:2015 REACH
5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile Chemical Properties
Boiling point
515.2±50.0 °C(Predicted)
density
1.37±0.1 g/cm3(Predicted)
storage temp.
Store at -20°C
solubility
Soluble in DMSO
form
crystalline solid
pka
13.42±0.10(Predicted)
Safety Information
MSDS Information
5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile Usage And Synthesis
Description
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F). Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma. AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro. It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM. AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 μM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.
Uses
AZ-960 Tyrosine Kinase inhibitor is useful for studying effects of the JAK2 Inhibitor, AZ960, on Pim??/BAD??/BCL-??xL survival signaling in the Human JAK2 V617F Cell Line SET-??2.
target
JAK2
5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile Preparation Products And Raw materials