R788 disodium hexahydrate

R788 disodium hexahydrate (CAS No.: 914295-16-2) is an orally administered prodrug. Its active metabolite, R406, is a potent spleen tyrosine kinase (Syk) inhibitor, with an IC50 of 41 nM against Syk in cell-free assays. Syk plays a key role in B-cell receptor (BCR) signaling; inhibition of Syk can block BCR-mediated signaling pathways, thereby affecting B-cell proliferation and survival. Studies show that R406 can inhibit the proliferation of multiple diffuse large B-cell lymphoma (DLBCL) cell lines, with EC50 values ranging from 0.8 μM to 8.1 μM. In in vivo studies, R788 is rapidly converted to R406 after oral administration, inhibiting Syk-dependent signaling pathways and thereby reducing immune complex-mediated inflammatory responses. In animal models, R788 has been used to investigate its therapeutic potential in B cell-related diseases, and the doses or concentrations used in experiments typically depend on the experimental design and research objectives.