AZ960

Additional information:
AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.|Product information|CAS Number: 905586-69-8|Molecular Weight: 354.36|Formula: C18H16F2N6|Chemical Name: 5-fluoro-2-[1-(4-fluorophenyl)ethyl]amino-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile|Smiles: CC1=CC(NC2N=C(NC(C)C3C=CC(F)=CC=3)C(=CC=2F)C#N)=NN1|InChiKey: SUNXHXDJOIXABJ-UHFFFAOYSA-N|InChi: InChI=1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 30 mg/mL (84.66 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|AZ960 inhibits Jak2 kinase with a Ki of 0.PMID:33289441 45 nM. Z960 possesses much less potent activity against Jak1, 3, and TYK2. AZ960 is active against other kinases, including TrkA, Aurora-A, and FAK, with IC50 of around 0.1 μM. AZ960 effectively 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. AZ960 potently inhibits the clonogenic growth and induces apoptosis of freshly isolated acute myelogenous leukemia cells from patients in association with cleavage of caspase 3 and down regulation of anti-apoptotic Bcl-xL proteins. AZ960 has a Ki of 1.25 μM for T. brucei extracellular signal-regulated kinase 8 (TbERK8). It inhibits TbERK8 with an IC50 of 120 nM.|Products are for research use only. Not for human use.|