Ifupinostat

Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research^[1]. IC50 & Target:IC50: <0.1 μM (PI3Kα)^[1] In Vitro:Ifupinostat (72 h) potently inhibits the viability of multiple hematological malignancy cell lines, with IC₅₀ values ranging from 0.7 to 30 nM after 72 h of treatment^[1].
Ifupinostat (8 nM; 24 h) inhibits PI3K/AKT/mTOR signaling, downregulates c-Myc and ferroptosis-related regulatory proteins in A20 and Daudi cells^[1].
Ifupinostat (8 nM; 48 h) induces accumulation of lipid ROS in A20 cells^[1].
Ifupinostat (8 nM; 48 h) reduces the GSH/GSSG ratio in A20 cells, promoting ferroptosis^[1]. In Vivo:Ifupinostat (100 mg/kg; intravenous injection; once every other day; 9 doses total) significantly inhibits the growth of various hematologic malignancy xenografts^[1].
Ifupinostat (25-100 mg/kg; intravenous injection; single dose) potently induces acetylation of histone H3 and inhibits phosphorylation of AKT in Daudi xenograft tumors^[1].
Ifupinostat (100 mg/kg; i.v.; administered every other day; 4 doses) induces tumor regression and significantly prolongs the survival of mice in an orthotopic brain lymphoma mouse model^[1].