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)

color 

Light yellow to yellow

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 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 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(905586-69-8)Related Product Information

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