AZ 960 [905586-69-8]

AdipoGen Life Sciences

AZ 960

10

905586-69-8

Research Use Only

>95%

C18H16F2N6

354.4

AZ-960 is a potent, selective and ATP-competitive JAK2 inhibitor that inhibits JAK2 kinase with a Ki of 0.45nM in vitro (3-fold selective over JAK3) and induces growth arrest and apoptosis in adult T cell leukemia (ATL) cells. 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 position 617 (V617F). Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma. AZ-960 induces growth arrest and apoptosis of human T cell lymphotropic virus type 1, HTLV-1-infected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of JAK2 and Bcl-2 family proteins including Bcl-2 and Mcl-1. 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 shows anti-parasitic activity through selective inhibition of the Trypanosoma brucei ERK8 inhibitor (TbERK8). - Chemical. CAS: 905586-69-8. Formula: C18H16F2N6. MW: 354.4. AZ-960 is a potent, selective and ATP-competitive JAK2 inhibitor that inhibits JAK2 kinase with a Ki of 0.45nM in vitro (3-fold selective over JAK3) and induces growth arrest and apoptosis in adult T cell leukemia (ATL) cells. 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 position 617 (V617F). Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma. AZ-960 induces growth arrest and apoptosis of human T cell lymphotropic virus type 1, HTLV-1-infected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of JAK2 and Bcl-2 family proteins including Bcl-2 and Mcl-1. 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 shows anti-parasitic activity through selective inhibition of the Trypanosoma brucei ERK8 inhibitor (TbERK8).

FC1=C(NC2=NNC(C)=C2)N=C(N[C@@H](C)C3=CC=C(F)C=C3)C(C#N)=C1

-20°C,2°C to 8°C

51202000