Bioactivity | Peficitinib (ASP015K) hydrobromide 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]. |
Invitro | 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]. Cell Proliferation Assay[1] Cell Line: |
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]. Animal Model: |
Name | Peficitinib hydrobromide |
CAS | 1353219-05-2 |
Formula | C18H23BrN4O2 |
Molar Mass | 407.30 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33. |