Peficitinib (hydrochloride)
CAS No. : 1353219-06-3
(Synonyms: ASP015K (hydrochloride); JNJ-54781532 (hydrochloride))
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| Cat. No. : | HY-19568B |
| M.Wt: | 362.85 |
| Formula: | C18H23ClN4O2 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].
IC50 & Target: IC50: 3.9 nM (JAK1), 5.0 nM (JAK2), 0.7 nM (JAK3), 4.8 nM (Tyk2)[1]
In Vitro: Peficitinib hydrobromide (0-100 nM; 3 days) inhibits IL-2-induced T cell proliferation in a concentration-dependent manner[1].
Peficitinib hydrobromide (10-1000 nM) inhibits IL-2-induced STAT5 phosphorylation in a concentration-dependent manner with a mean IC50 of 124 nM in rat whole blood, and inhibits STAT5 phosphorylation with a mean IC50 of 127 nM in human lymphocytes[1].
In Vivo: Peficitinib hydrobromide (1-30 mg/kg; p.o.; once daily for 24 days) shows dose-dependent efficacy both in prophylactic and therapeutic dosing regimens in an adjuvant-induced arthritis rat model[1].
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