Brepocitinib 是JAK1和TYK2双重抑制剂，IC50分别为 17 nM 和 23 nM。它抑制JAK2和JAK3的效果较弱，IC50分别为 77 nM 和 6.49 μM 。

Brepocitinib is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). Brepocitinib also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).

PF-06700841 inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood IC50s: 65/120 nM). PF-06700841 inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (IC50s: 238/204 nM). PF-06700841 also has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50: 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50: 641 nM). PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50: 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 (IC50s: 305 nM/86 nM).

PF-06700841 (3-30 mg/kg; p.o; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with PF-06700841 at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM.

1883299-62-4

C18H21F2N7O

389.4

PF-06700841

H2O:Insoluble
DMSO:75 mg/mL (192.60 mM)
H2O:Insoluble
Ethanol:75 mg/mL (192.60 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years