Art. -Nr.: HY-19568

Peficitinib

(Synonyms: ASP015K; JNJ-54781532)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

Peficitinib (ASP015K) 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.

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Reinheit: 99.38%
CAS. Nr.: 944118-01-8
Formel: C₁₈H₂₂N₄O₂
Molecular Weight:326.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Peficitinib Chemical Structure

CAS. Nr.: 944118-01-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Peficitinib (ASP015K) 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)

Alle JAK Isoform-spezifische Produkte anzeigen :

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 944118-01-8
Appearance Solid
Molecular Weight 326.39
Formel C₁₈H₂₂N₄O₂
Color Light yellow to yellow
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
Synonyms

ASP015K; JNJ-54781532
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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 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 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 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 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 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 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 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.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 58.33 mg/mL (178.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0638 mL

15.3191 mL

30.6382 mL

5 mM

0.6128 mL

3.0638 mL

6.1276 mL

10 mM

0.3064 mL

1.5319 mL

3.0638 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[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]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0638 mL	15.3191 mL	30.6382 mL	76.5955 mL
	5 mM	0.6128 mL	3.0638 mL	6.1276 mL	15.3191 mL
	10 mM	0.3064 mL	1.5319 mL	3.0638 mL	7.6595 mL
	15 mM	0.2043 mL	1.0213 mL	2.0425 mL	5.1064 mL
	20 mM	0.1532 mL	0.7660 mL	1.5319 mL	3.8298 mL
	25 mM	0.1226 mL	0.6128 mL	1.2255 mL	3.0638 mL
	30 mM	0.1021 mL	0.5106 mL	1.0213 mL	2.5532 mL
	40 mM	0.0766 mL	0.3830 mL	0.7660 mL	1.9149 mL
	50 mM	0.0613 mL	0.3064 mL	0.6128 mL	1.5319 mL
	60 mM	0.0511 mL	0.2553 mL	0.5106 mL	1.2766 mL
	80 mM	0.0383 mL	0.1915 mL	0.3830 mL	0.9574 mL
	100 mM	0.0306 mL	0.1532 mL	0.3064 mL	0.7660 mL

Keywords

Peficitinib

11 Cited Publications

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Peficitinib

Epigenetics Compound Library

Immunology/Inflammation Compound Library

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Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Publications Citing Use of MedChemExpress (MCE) Peficitinib

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Peficitinib Related Classifications

HY-19568 Related Classifications