RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.
RSH-7 (1-1000 nM; 72 h) shows antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively[1].RSH-7 (30, 150, 750 nM; 72 h) decreases the expression of p-BTK (TYR223), p-PLCγ(Tyr1217), p-FLT3 (Tyr589), p-STAT5 (TYR694) in a dose-dependent manner[1].RSH-7 (30, 150, 750 nM; 72 h) induces apoptosis and increases the expression of BAX, p53, cleaved caspase 3 in a dose dependen manner in jeko-1 cells[1].
RSH-7 (25, 50 mg/kg; i.p.; daily for 16 days) shows anti-tumor activity with significantly and dose-dependently suppresses the tumor growth in mouse[1].
References:
[1]. Ran F, et al. Development of novel drazidoarylaminopyrimidine-based BTK/FLT3 dual inhibitors with potent in vivo anti-hematological malignancies effects. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114913.