Biochem/physiol Actions
ATP-competitive, potent and selective Janus-associated kinase 2 (JAK2) inhibitor.
AZ960 is an ATP-competitive, potent and selective Janus-associated kinase 2 inhibitor (JAK2 Ki = 0.45 nM with 15 μM ATP, 96% inhibition at 10 nM) with additional lower potency against TrkA/Aurora-A/ARK5 (91/73/65% inhibition at 10 nM; IC50 >100 nM against 72 other kinases). AZ960 exhibits JAK2-selective anti-proliferation potency (GI50 = 25, 214, 230, 279 nM using cells expression TEL-JAK2, -Tyk2, -JAK1, -JAK3, respectively) and inhibits cellular STAT5 phosphorylation in TEL-JAK2-expressing cells (IC50 = 15 nM) at a 15–30-fold potency than the TEL-JAK1, -JAK3, and -Tyk2 transfectants.