bs-75632C

DATASHEET

Formulation Solid

Storage: Stable for 2 years after receipt when stored at -20°C.

Product Information:

CAS Number: 905586-69-8

Molecular formula: C18H16F2N6

Molecular weight: 354.4

Purity: >95%

Appearance: White to off-white solid.

Solubility: Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (2mg/ml).

InChiKey: SUNXHXDJOIXABJ-NSHDSACASA-N

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

Description:

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).