BET-IN-14 is an orally active pan BET inhibitor with an IC50 of 5.35 nM. It exhibits anti-cancer activity. In vitro studies show that BET-IN-14 (Compound 171) has anti-tumor activity against various cancer cell lines (average IC50: 174.7 nM), particularly in MM.1S, Ty-82, MV-4-11, and KG-1 cells. In vivo, BET-IN-14 (50 and 100 mg/kg, p.o., qd) inhibits tumor growth in MV-4-11 xenograft models by 60.36%.
- Orally active pan BET inhibitor with high potency (IC50 of 5.35 nM)
- Displays anti-tumor activity against various cancer cell lines (average IC50: 174.7 nM)
- Effective in MM.1S, Ty-82, MV-4-11, and KG-1 cells
- Inhibits tumor growth in MV-4-11 xenograft models by over 60% at tested dosages