1229236-86-5

LY2784544 is a JAK2 inhibitor. LY2784544 may be used as a potential treatment for patients with myeloproliferative neoplasm.

ChEBI: Gandotinib is a member of pyridazines.

LY2784544 is an orally activeATP-competitivepotent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 μM/JAK219.8 nM/20 μM/JAK148.0 nM/2 μM/JAK3) with little activity toward 79 other kinases. LY2784544 selectively inhibits signaling/proliferation driven by oncogenic JAK2V617F (IC50 = 20/55 nM) over those mediated by wt JAK2 upon IL-3 induction (IC50 = 1183/1309 nM) in Ba/F3 cultures and displays in vivo efficacious in a JAK2V617F-induced murine MPN model (10-80 mg/kg bid po.). LY2784544 is also reported to display Zn-dependent (optimal [Zn+2] = 100 μM) GPR39 agonist activitybut not 11 other GPRs.

wild-type JAK2

JAK2: 3 nM (IC₅₀); Tyk2: 44 nM (IC₅₀); JAK3: 48 nM (IC₅₀); FGFR2: 32 nM (IC₅₀); FGFR3: 106 nM (IC₅₀); Flt-4: 25 nM (IC₅₀); KDR: 109 nM (IC₅₀); FLT3: 4 nM (IC₅₀); TRKB: 95 nM (IC₅₀); ALK: 138 nM (IC₅₀); MUSK: 147 nM (IC₅₀); AURKA: 168 nM (IC₅₀); MAP3K9: 299 nM (IC₅₀)