Catalog No.: PC-38049Not For Human Use, Lab Use Only.
GDC-046 is a potent, selective, and orally bioavailable inhibitor of TYK2 with with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
GDC-046 is a potent, selective, and orally bioavailable inhibitor of TYK2 with with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) in cell based assays.
GDC-046 also displays less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM), and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM).
GDC-046 shows statistically significant knockdown of cytokine interferon-γ (IFNγ), in a mouse IL-12 PK/PD model.
