2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. Peficitinib

Peficitinib  (Synonyms: ASP015K; JNJ-54781532)

Cat. No.: HY-19568 Purity: 99.25%
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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.

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

Peficitinib Chemical Structure

Peficitinib Chemical Structure

CAS No. : 944118-01-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 83 In-stock
Solution
10 mM * 1 mL in DMSO USD 83 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 75 In-stock
10 mg USD 130 In-stock
50 mg USD 370 In-stock
100 mg USD 610 In-stock
200 mg   Get quote  
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Peficitinib:

Peficitinib Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    View All JAK Isoform Specific Products:

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    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    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)

    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.

    Peficitinib Related Antibodies

    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
    Molecular Weight

    326.39

    Formula

    C18H22N4O2
    CAS No.
    Appearance

    Solid

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 60 mg/mL (183.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0638 mL 15.3191 mL 30.6382 mL
    5 mM 0.6128 mL 3.0638 mL 6.1276 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.43%

    COA (251 KB) HNMR (181 KB) LCMS (320 KB)

    Handling Instructions (2659 KB)
    References

    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
    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
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    Peficitinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Peficitinib944118-01-8ASP015K JNJ-54781532JNJ54781532JNJ 54781532JNJ-54781532JAKJanus kinaserheumatoid arthritisIL-2splenocyteslymphocytesInhibitorinhibitorinhibit

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