Description
A Syk inhibitor (Ki = 7.5 nM); selective for Syk over Lyn, Fyn, Src, Itk, and BTK (Kis = >4.7 µM for all); inhibits anti-IgE-induced histamine release in isolated human mast cells sensitized with IgE (IC50 = 5.1 nM); reduces anti-IgM-induced proliferation of isolated mouse splenic B cells (IC50 = 58 nM); sensitizes MCF-7 human breast cancer cells to TRAIL-induced apoptosis from 0.31-2.5 µM; inhibits passive cutaneous anaphylaxis in rats (ED50 = 8 mg/kg); reduces tumor growth in an MCF-7 mouse xenograft model at 50 mg/kg alone or in combination with TRAIL