XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC 50 of 11.4 nM[1]. XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC 50 values of 326.6 nM, 685.6 nM and 1065 nM, respectively[1]. XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC 50 of 182.3 nM against BTK(C481S)-Ba/F3 cells[1]. XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells[1]. XMU-MP-3 (10-1000 nM; 4 hours) inhibits both the auto- and trans-phosphorylation of BTK at the site of Y223 and Y551 in a dose-dependent manner in BTK-transformed Ba/F3 cells[1]. Cell Proliferation Assay[1]Cell Line: BTK-transformed and parental Ba/F3 cells Concentration: 0.001, 0.01, 0.1, 1, 10, 100, 1000, 10000 nM Incubation Time: 48 hours Result: Inhibited BTK-transformed Ba/F3 cell proliferation with an IC 50 of 11.4 nM, while it showed negligible anti-proliferative effects on parental wild-type Ba/F3 cells (IC 50 >10000 nM). Western Blot Analysis[1]Cell Line: BTK-transformed Ba/F3 cells Concentration: 10, 50, 100, 500, 1000 nM Incubation Time: 4 hours Result: The phosphorylation levels of BTK Y223 and Y551 were reduced significantly at concentrations as low as 100 nM, and completely suppressed at the concentration of 1000 nM.

XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models[1]. Animal Model: Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models[1]Dosage: 25 and 50 mg/kg Administration: Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days Result: Significantly reduced the tumor size without affecting animal weights.