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 K
i 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 GI
50 value of 33 nM. AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-
infected (IC
50 = ~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.
![5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile Structure](https://www.chemicalbook.com/CAS2/GIF/905586-69-8.gif)
