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Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Peficitinib suppresses the IL-2-induced proliferation of human T cells with greater potency than EPO-induced proliferation of human erythroleukemia cells. In human whole blood, ASP015K inhibits STAT5 phosphorylation (pSTAT5).
In vivo, Peficitinib (20 mg/kg, p.o.) suppresses IL-2-induced STAT5 phosphorylation by 78% in the rat model of adjuvant-induced arthritis (AIA). Peficitinib potently inhibits the increase in paw volume (≥1 mg/kg) with an ED50 of 2.7 mg/kg, significantly reduces the bone destruction score (≥10 mg/kg) and almost fully ameliorates both paw swelling and bone destruction scores (30 mg/kg).
| Molecular Weight | 326.39 |
| Formula | C18H22N4O2 |
| CAS Number | 944118-01-8 |
| Solubility (25°C) | DMSO: ≥ 55 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Yuko Kaneko. Efficacy and safety of peficitinib in rheumatoid arthritis
[4] Anthony Markham, et al. Peficitinib: First Global Approval
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| Momelotinib (CYT387)
Momelotinib (CYT387) is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively. |
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