AZ960 is a potent, selective JAK2 inhibitor with Ki of 0.45 nM, IC50 of <3 nM.
AZ960 displays 3-fold selectivity over JAK3 (IC50=9 nM).
AZ960 blocks STAT5 phosphorylation and potently inhibits cell proliferation (GI50=25 nM) in TEL-JAK2 driven Ba/F3 cells, blocks BCL-XL, PIM1 and PIM2 mRNA expression and induces apoptosis; also induces growth arrest and apoptosis in adult T-cell leukemia cells.
AZ960 also inhibits parasite Trypanosoma brucei ERK8 (Ki=1.25 uM) with antiparasitic activity (IC50=120nM).
