Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). Brepocitinib also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 38.00 | |
2 mg | In stock | $ 54.00 | |
5 mg | In stock | $ 89.00 | |
10 mg | In stock | $ 147.00 | |
25 mg | In stock | $ 313.00 | |
50 mg | In stock | $ 478.00 | |
100 mg | In stock | $ 688.00 | |
200 mg | In stock | $ 957.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 119.00 |
Description | Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). Brepocitinib also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM). |
Targets&IC50 | JAK2:77 nM (cell free), JAK1:17 nM (cell free), TYK2:23 nM (cell free), JAK3:6.9 μM |
In vitro | 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). |
In vivo | 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. |
Synonyms | PF-06700841 |
Molecular Weight | 389.4 |
Formula | C18H21F2N7O |
CAS No. | 1883299-62-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 75 mg/mL (192.60 mM)
DMSO: 75 mg/mL (192.60 mM)
H2O: Insoluble
You can also refer to dose conversion for different animals. More
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Brepocitinib 1883299-62-4 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK inhibit Janus kinase PF-06700841 Inhibitor PF06700841 PF 06700841 inhibitor