1353219-06-3

1353219-06-3 structure

1353219-06-3 structure

Name: Peficitinib hydrochloride
Chemical Name: Peficitinib hydrochloride
CAS Number: 1353219-06-3
Molecular Formula: C₁₈H₂₃ClN₄O₂
Molecular Weight: 362.85
Catalog: Signaling Pathways Epigenetics JAK
Create Date: 2022-10-15 11:25:06
Modify Date: 2024-01-10 00:26:39
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].

Name	Peficitinib hydrochloride

Description	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].
Related Catalog	Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK Research Areas >> Inflammation/Immunology
Target	JAK3:0.7 nM (IC50) JAK1:3.9 nM (IC50) Tyk2:4.8 nM (IC50) JAK2:5 nM (IC50)
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]. Cell Proliferation Assay[1] Cell Line: Splenocytes from male Lewis rats Concentration: 0-100 nM Incubation Time: 3 days Result: Inhibited IL-2-induced T cell proliferation in a concentration-dependent manner with an IC50 of 10 nM.
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: Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model[1] Dosage: 1, 3, 10, and 30 mg/kg Administration: Oral administration, once daily for 24 days Result: Significantly inhibited the increase in paw volume at doses of 1 mg/kg or greater with an ED50 value of 2.7 mg/kg (95% confidence interval: 1.5–4.2 mg/kg). Significantly reduced the bone destruction score at 10 mg/kg or greater and almost fully ameliorated both paw swelling and bone destruction scores at 30 mg/kg.
References	[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.

Molecular Formula	C₁₈H₂₃ClN₄O₂
Molecular Weight	362.85