Flonoltinib TFA is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib TFA has anti-cancer activity [1].
In Vivo, Flonoltinib (30 and 60 mg/kg/day; p.o.; for 14 days) TFA exhibits significant antitumor effects[1].
In Vitro, Flonoltinib (0.008-1 μM; for 2 hours) TFA down-regulates p-FLT3 in a dose-dependent manner[1]. Flonoltinib (5-100 nM; for 2 hours) TFA has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1]. Flonoltinib (5-100 nM; for 2 hours) TFA strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].
References:
[1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.
In Vivo, Flonoltinib (30 and 60 mg/kg/day; p.o.; for 14 days) TFA exhibits significant antitumor effects[1].
In Vitro, Flonoltinib (0.008-1 μM; for 2 hours) TFA down-regulates p-FLT3 in a dose-dependent manner[1]. Flonoltinib (5-100 nM; for 2 hours) TFA has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1]. Flonoltinib (5-100 nM; for 2 hours) TFA strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].
References:
[1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.