Peficitinib hydrobromide

Modify Date: 2024-01-11 18:31:03

Peficitinib hydrobromide structure	Common Name	Peficitinib hydrobromide
	CAS Number	1353219-05-2	Molecular Weight	407.30
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₈H₂₃BrN₄O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Peficitinib hydrobromide

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.

Name	Peficitinib hydrobromide

Description	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.
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) JAK2:5 nM (IC50) Tyk2:4.8 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	C₁₈H₂₃BrN₄O₂
Molecular Weight	407.30