Peficitinib

SKU: orb1223560

Description

Peficitinib (ASP-015K, JNJ-54781532) is a potent JAK inhibitor with IC50s of 3.9 and 0.7 nM for JAK1 and JAK3 respectively; inhibits IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo; dose-dependently suppresses bone destruction and paw swelling in an adjuvant-induced arthritis model in rats; orally bioactive.Rheumatoid Arthritis Phase 3 Clinical.

Images & Validation

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Key Properties

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CAS Number	944118-01-8
MW	326.3929
Purity	>98% (HPLC)
Formula	C₁₈H₂₂N₄O₂
SMILES	C1C2CC3CC(C2)(CC1C3NC4=C5C=CNC5=NC=C4C(=O)N)O
Target	JAK
Solubility	DMSO: ≥ 60 mg/mL

Bioactivity

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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. Animal model: Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model. 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.

In Vitro

Peficitinib hydrobromide (0-100 nM; 3 days) inhibits IL-2-induced T cell proliferation in a concentration-dependent manner. 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. Cell Proliferation Assay 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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ASP-015K | JNJ-54781532

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JAK

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Peficitinib (orb1223560)

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CAS Number:	1353219-06-3
MW:	362.86
Formula:	C₁₈H₂₃ClN₄O₂

Purity:	99.84%
CAS Number:	944118-01-8
MW:	326.39
Formula:	C₁₈H₂₂N₄O₂

CAS Number:	1353219-05-2
MW:	407.312
Formula:	C₁₈H₂₃BrN₄O₂

Peficitinib

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Peficitinib hydrochloride [orb1688672]

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Peficitinib hydrobromide [orb1695731]

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Peficitinib (orb1223560)

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