Molecular Formula | C18H21F2N7O |
Molar Mass | 389.4 |
Density | 1.63±0.1 g/cm3(Predicted) |
Boling Point | 637.1±65.0 °C(Predicted) |
Appearance | powder |
Color | white to beige |
pKa | 7.28±0.10(Predicted) |
Storage Condition | room temp |
In vivo study | PF-06700841 pharmacokinetic studies in Sprague − Dawley rats after intravenous injection of 1 mg/kg PF-06700841 tosylate or oral administration of 3 mg/kg PF-06700841 tosylate, the plasma clearance of PF-06700841 in vivo was 31 mL/min/kg, the volume of distribution was 2.0 L/kg, and its oral bioavailability was 83%. After oral administration of 3 mg/kg, its Cmax was 774 ng/mL and auc∞ was 1340 ng · h/mL. The high oral bioavailability of PF-06700841 indicates that it has a high intestinal Absorbability, which is associated with its passive osmotic activity and high solubility in vitro. |
biological activity | PF-06700841 (PF-841) is a potent Tyk2 and Jak1 inhibitor, the IC50 for Jak1 and Jak2 are 23 nM, 17 nM and 77 nM, respectively. |
Target | Value |
JAK1 (Cell-free assay) | 17 nM |
Tyk2 (Cell-free assay) | 23 nM |
JAK2 (Cell-free assay) | 77 nM |