AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
IC50&Target
JAK2
0.45 nM (Ki)
JAK2
<3 nM (IC50)
JAK3
9 nM (IC50)
体外研究
AZ960 inhibits Jak2 kinase with a Ki of 0.45 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.
分子式
C18H16F2N6
分子量
354.36
CAS号
905586-69-8
运输条件
Room temperature in continental US; may vary elsewhere.