A potent JAK2 inhibitor (Ki = 0.45 nM in vitro) that decrease STAT3/5 phosphorylation and inhibits cell proliferation (GI50 = 33 nM) in a JAK2 V617F mutated cell line; induces apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM)

AZ 960 – 10 mg

Brand:
Cayman
CAS:
905586-69-8
Storage:
-20
UN-No:
Non-Hazardous - /

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).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} 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.{27171} 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.{27172}  

 

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Description

A potent JAK2 inhibitor (Ki = 0.45 nM in vitro) that decrease STAT3/5 phosphorylation and inhibits cell proliferation (GI50 = 33 nM) in a JAK2 V617F mutated cell line; induces apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), downregulating phosphorylated forms of JAK2 and Bcl-2 family proteins

Formal name: 5-fluoro-​2-​[[(1S)-​1-​(4-​fluorophenyl)​ethyl]​amino]​-​6-​[(5-​methyl-​1H-​pyrazol-​3-​yl)​amino]-3-pyridinecarbonitrile

Synonyms: 

Molecular weight: 354.4

CAS: 905586-69-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Signaling|JAK Signaling

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