Flonoltinib maleate is an orally effective dual JAK2/FLT3 inhibitor, with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. Known as JAK2/FLT3-IN-1, it exhibits anticancer activity.

JAK3:39 nM, JAK1:26 nM, JAK2:0.7 nM

Flonoltinib maleate (0.008-1 μM; for 2 hours) dose-dependently downregulates p-FLT3. Additionally, Flonoltinib maleate (5-100 nM; for 2 hours) exhibits a dose-dependent induction of apoptosis in MV4-11 cells. At a concentration of 100 nM, Flonoltinib maleate significantly induces cell cycle arrest, with an 85% increase in the G1/G0 phase in MV4-11 cells.

Flonoltinib maleate, administered orally at doses of 30 and 60 mg/kg/day over a continuous period of 14 days, demonstrated significant antitumor activity.