Peficitinib
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.38%
- No. CAS: 944118-01-8
- Fòrmula: C18H22N4O2
- Peso molecular:326.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Peficitinib
More- Sci Adv. 2024 Mar 22;10(12):eadl0368. [Abstract]
- Talanta. 2020 Feb 1;208:120450. [Abstract]
- Biochem Pharmacol. 2025 Oct:240:117120. [Abstract]
- Biochem Pharmacol. 2025 Jan 9:116744. [Abstract]
- Inflamm Res. 2025 Apr 29;74(1):72. [Abstract]
- Cells. 2019 Jun 9;8(6). pii: E561. [Abstract]
- Eur J Pharmacol. 2024 Dec 5:984:177020. [Abstract]
- Int Immunopharmacol. 2024 May 10:132:111931. [Abstract]
- mSphere. 2025 Nov 25;10(11):e0068125. [Abstract]
- J Biochem Mol Toxicol. 2025 Jan;39(1):e70097. [Abstract]
- Cancer Manag Res. 2018 Dec 28:11:389-399. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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ELISA
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In Vivo Efficacy Study
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RT-PCR
Actividad biológica
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JAK3 0.7 nM (IC50) |
JAK1 3.9 nM (IC50) |
Tyk2 4.8 nM (IC50) |
JAK2 5 nM (IC50) |
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.
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Cell Line:Splenocytes from male Lewis rats
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Concentration:0-100 nM
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Incubation Time:3 days
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Result:Inhibited IL-2-induced T cell proliferation in a concentration-dependent manner with an IC50 of 10 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model[1]
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Dosage:1, 3, 10, and 30 mg/kg
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Administration:Oral administration, once daily for 24 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 944118-01-8
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Appearance Solid
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Peso molecular 326.39
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Fòrmula C18H22N4O2
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Color Light yellow to yellow
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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
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Synonyms
ASP015K; JNJ-54781532
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Sci Adv
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.
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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.
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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.
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Eur J Pharmacol
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.
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |
Peficitinib Related Classifications
HY-19568 Related Classifications
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