NS-018 (maleate)

Biological Activity

Ilginatinib maleate (NS-018 maleate) is a highly potent, orally available JAK2 inhibitor with IC50 of 0.72 nM, 46-fold selectivity for JAK1 (IC50, 33 nM) and 54-fold for JAK3 ( IC50, 39 nM), and 22 times that of Tyk2 (IC50, 22 nM).

in vivo

Ilginatinib maleate (NS-018 maleate) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model.

target

JAK2 0.72 nM (IC 50 )

Tyk2 22 nM (IC 50 )

JAK1 33 nM (IC 50 )

JAK3 39 nM ( IC 50 )