Table 8. In vitro Biological Profile of BIIB129 (25).
| assay format (cell type, stimulus) | readout |
|---|---|
| kinact/Ki (purified nonphosphorylated BTK protein) | 6 M–1 s–1 |
| TO50 (TMD8 cells) | 6.8 nM |
| IC50 PLCγ2 phosphorylation (Ramos cells, IgM) | 1.2 nM |
| IC50 activation and translocation of NF-κB (TMD8) | 1.9 nM |
| IC50 B cell activation (PBMCs anti-IgD/BCR) | 13 nM |
| IC50 TMD8 proliferation (CD19 and CD36 expression) | 4.2 and 1.2 nM |
| IC50 blocking FcγR-induced TNF secretion (monocytes) | 3.0 nM |
| IC50 B cell-mediated antigen presentation to T cells | 1.9 nM |