Ruserontinib

Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC₅₀ value of 55 nM for human FLT3, and has antitumor activity^[1]. In Vitro: Ruserontinib (SKLB1028) can significantly inhibit the growth of mf4-11 cells expressing FLT3-ITD with IC₅₀ value of 0.002 μM, inhibit the proliferation of RS4-11 cells expressing wt-FLT3 with IC₅₀ value of 0.790 μM, and inhibit Ba The IC₅₀ value for the growth of /F3 cells is 0.01 μM, and the IC₅₀ value for inhibiting the growth of K562 cells expressing the Bcr-Abl mutant is 0.190 μM^[1].
Ruserontinib (SKLB1028) (0-100 nM, 20 h) causes a dose-dependent decrease in the level of pro-caspase-3 in MV4-11 cells, while a dose-dependent increase in the level of the cleaved caspase-3 fragment, and can be dose-dependent Inhibits phosphorylation of STAT5 and Erk1/2 in a dependent manner^[1].
In Vivo: Ruserontinib (SKLB1028) (5-70 mg/kg, orally once daily, 18 days) have anti-tumor effect in MV4-11 and K562 xenograft NOD-SCID models^[1].