Cat. No.: HY-19568B

Peficitinib hydrochloride

(Synonyms: ASP015K hydrochloride; JNJ-54781532 hydrochloride)

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

CAS No.: 1353219-06-3
Formula: C₁₈H₂₃ClN₄O₂
Molecular Weight:362.85

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

Peficitinib hydrochloride Chemical Structure

CAS No.: 1353219-06-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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].

IC₅₀ & Target^[1]

JAK3

0.7 nM (IC₅₀)

JAK1

3.9 nM (IC₅₀)

Tyk2

4.8 nM (IC₅₀)

JAK2

5 nM (IC₅₀)

All JAK Isoforms :

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 1353219-06-3
Molecular Weight 362.85
Formula C₁₈H₂₃ClN₄O₂
SMILES

O[C@](C[C@@H]1C[C@H]2C3)(C2)C[C@@H]3[C@H]1NC4=C5C(NC=C5)=NC=C4C(N)=O.Cl
Synonyms

ASP015K hydrochloride; JNJ-54781532 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (11)

All Cell Proliferation/Viability AssayCell Imaging/StainingELISAIn Vivo Efficacy StudyRT-PCRWB

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Journal Impact Factor

Sci Adv

JAK/STAT signaling pathway affects CCR5 expression in human CD4+ T cells. [Abstract]

2024 Mar 22;10(12):eadl0368. PMID: 38507500
Talanta

Effective quantification of 11 tyrosine kinase inhibitors and caffeine in human plasma by validated LC-MS/MS method with potent phospholipids clean-up procedure. Application to therapeutic drug monitoring. [Abstract]

2020 Feb 1;208:120450. PMID: 31816725
Biochem Pharmacol

Dual inhibition of EGR1/STAT3 transcriptional hubs suppresses macrophage-driven liver fibrosis: A multi-omics-guided drug repurposing strategy. [Abstract]

2025 Oct:240:117120. PMID: 40623460

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Oct:240:117120. [Abstract]

Peficitinib (3 μM; 24 h) significantly attenuated HSC activation when compared to IL-4-induced M2 macrophages alone.

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Oct:240:117120. [Abstract]

Peficitinib (3 μM; 24 h) led to a reduction in TGF-β secretion of IL-4-induced M2 macrophages.

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Oct:240:117120. [Abstract]

Peficitinib (3 μM; 24 h) significantly downregulated M2 polarization markers Cd206, Arg1, nuclear transcription factors Egr1, Stat3, pro-fibrotic mediators Fn1, Thbs1, Spp1, and HSC activation markers Acta2, Col1a1 at the mRNA level in IL-4-induced M2 macrophages.
Biochem Pharmacol

Direct reprogramming of human fibroblasts into hair-inducing dermal papilla cell-like cells by a single small molecule. [Abstract]

2025 Jan 9:116744. PMID: 39798934

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Jan 9:116744. [Abstract]

Peficitinib (10 μM; 8 d) induced cell enlargement and rounding and elevated ALP expression in human foreskin fibroblasts.

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Jan 9:116744. [Abstract]

Peficitinib (10 μM; 8 d) induced significant hair growth of BALB/c-nu/nu mice.
Inflamm Res

The IL-6 autocrine loop promoting IFN-γ-induced fibroblast senescence is involved in psychological stress-mediated exacerbation of vitiligo. [Abstract]

2025 Apr 29;74(1):72. PMID: 40299037
Cells

Peficitinib Inhibits the Chemotactic Activity of Monocytes via Proinflammatory Cytokine Production in Rheumatoid Arthritis Fibroblast-Like Synoviocytes. [Abstract]

2019 Jun 9;8(6). pii: E561. PMID: 31181818

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cells. 2019 Jun 9;8(6). pii: E561. [Abstract]

Effects of Peficitinib on IL-6 and IL-6R responses in RA FLS. The RA FLS are stimulated with IL-6 (100 ng/mL) and IL-6R (100 ng/mL) after treating with Peficitinib (0.1, 1, 5 μM) for 24 h. Representative western blot images showed that peficitinib suppressed the phosphorylation of STAT1, STAT3, and STAT5 in RA FLS.
Eur J Pharmacol

Peficitinib halts acute kidney injury via JAK/STAT3 and growth factors immunomodulation. [Abstract]

2024 Dec 5:984:177020. PMID: 39349115
Int Immunopharmacol

Peficitinib alleviated acute lung injury by blocking glycolysis through JAK3/STAT3 pathway. [Abstract]

2024 May 10:132:111931. PMID: 38547769
mSphere

The Pseudomonas aeruginosa effector protein TesG regulates alternative activation of macrophages through NLRC5. [Abstract]

2025 Nov 25;10(11):e0068125. PMID: 41170846
J Biochem Mol Toxicol

TFAP2A Activates ADAM8 to Promote Lung Adenocarcinoma Angiogenesis Through the JAK/STAT Signaling Pathway. [Abstract]

2025 Jan;39(1):e70097. PMID: 39812116
Cancer Manag Res

OCT4 accelerates tumorigenesis through activating JAK/STAT signaling in ovarian cancer side population cells. [Abstract]

2018 Dec 28:11:389-399. PMID: 30643464

Peficitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Manag Res. 2018 Dec 28:11:389-399. [Abstract]

Western blotting analysis of the protein levels of JAK1 and caspase-3 in different treated NSP cells: Lentiv-NC (48 hours), Lentiv-OCT4 (48 hours), and peficitinib (4.8 nM, 2 hours) + Lentiv-OCT4 (48 hours). Left: SKOV3 cells, right: A2780 cells.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Peficitinib hydrochloride

11 Cited Publications

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Peficitinib hydrochloride

Publications Citing Use of MedChemExpress (MCE) Peficitinib hydrochloride

All JAK Isoforms

Biological Activity

Chemical Information

Publications (11)

Purity & Documentation

References

Calculators

Help & FAQs

Peficitinib hydrochloride Related Classifications

HY-19568B Related Classifications