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: 99.23%
COA Handling Instructions

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

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10 mM * 1 mL in DMSO USD 103 In-stock
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10 mM * 1 mL
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10 mg USD 165 In-stock
50 mg USD 495 In-stock
100 mg USD 825 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Peficitinib:

Peficitinib Related Antibodies

Top Publications Citing Use of Products

    Peficitinib purchased from MCE. 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 MCE. 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.

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    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

    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].

    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

    Appearance

    Solid

    Formula

    C18H22N4O2
    CAS No.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 60 mg/mL (183.83 mM)

    *"≥" 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
    10 mM 0.3064 mL 1.5319 mL 3.0638 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.43%

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

    Handling Instructions (2659 KB)
    References
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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.

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    Keywords:

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

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