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

Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.

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

CAS No. : 1622902-68-4

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Abrocitinib:

Abrocitinib Related Antibodies

Top Publications Citing Use of Products

    Abrocitinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Jan 22;17(1):619.  [Abstract]

    Cell viability assays in MCF7 Par and PR, T47D Par and PR, and MDA-MB-231 Par and PR cells treated with Abrocitinib (ABR) (1 μM; 5 d).

    Abrocitinib purchased from MedChemExpress. Usage Cited in: Clin Immunol. 2025 Dec 2:283:110654.  [Abstract]

    The JAK1 inhibitor Abrocitinib (300 μM) abolished ISG15 induction upon stimulation of PBMCs with R848, poly I:C, and CpG A.

    Abrocitinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 May 25;24(11):9243.

    Abrocitinib (50-200 nM; 24 h) significantly decreased VV (poxvirus) plaque number in IL-4 + IL-13-treated KC cultures.

    Abrocitinib purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2022 Feb:119:105538.

    Abrocitinib (AB) (7.5 mg/kg; i.g.; once daily for 14 d) reduced the protein expression of TSLP and IVL, while up-regulated the protein expressions of FLG and LOR in dorsal skin of the DNCB-treated mice.

    Abrocitinib purchased from MedChemExpress. Usage Cited in: Bioorg Chem. 2022 Feb:119:105538.

    Abrocitinib (AB) (7.5 mg/kg; i.g.; once daily for 14 d) significantly decreased the ratio of p-IκBα/IκBα and p-p65/p65, and increased the expression level of IκBα in the nucleus in the dorsal skin of the DNCB-treated mice.

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    • Biological Activity

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    Description

    Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease[1].

    IC50 & Target[1]

    JAK1

    29 nM (IC50)

    JAK2

    803 nM (IC50)

    Tyk2

    1253 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    TF-1 IC50
    1.4 μM
    Compound: Abrocitinib
    Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay
    Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay
    		[PMID: 32462873]
    In Vitro

    Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively[1].

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

    Abrocitinib Related Antibodies
    In Vivo

    Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model[1].

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

    Animal Model: Female Lewis rats (8−10 weeks old)[1]
    Dosage: 5, 15, 50 mg/kg
    Administration: P.O. daily for 7 days
    Result: Obviously reduced paw swelling at all doses.
    Clinical Trial
    Molecular Weight

    323.41

    Formula

    C14H21N5O2S
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CN([C@H]1C[C@@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2
    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 : 100 mg/mL (309.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0921 mL 15.4603 mL 30.9205 mL
    5 mM 0.6184 mL 3.0921 mL 6.1841 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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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.08 mg/mL (6.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  0.5% CMC-Na/saline water

      Solubility: 3.64 mg/mL (11.26 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    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: 99.26%

    SDS (396 KB)

    COA (246 KB) LCMS (268 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 3.0921 mL 15.4603 mL 30.9205 mL 77.3013 mL
    5 mM 0.6184 mL 3.0921 mL 6.1841 mL 15.4603 mL
    10 mM 0.3092 mL 1.5460 mL 3.0921 mL 7.7301 mL
    15 mM 0.2061 mL 1.0307 mL 2.0614 mL 5.1534 mL
    20 mM 0.1546 mL 0.7730 mL 1.5460 mL 3.8651 mL
    25 mM 0.1237 mL 0.6184 mL 1.2368 mL 3.0921 mL
    30 mM 0.1031 mL 0.5153 mL 1.0307 mL 2.5767 mL
    40 mM 0.0773 mL 0.3865 mL 0.7730 mL 1.9325 mL
    50 mM 0.0618 mL 0.3092 mL 0.6184 mL 1.5460 mL
    60 mM 0.0515 mL 0.2577 mL 0.5153 mL 1.2884 mL
    80 mM 0.0387 mL 0.1933 mL 0.3865 mL 0.9663 mL
    100 mM 0.0309 mL 0.1546 mL 0.3092 mL 0.7730 mL
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    Abrocitinib 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:

    Abrocitinib1622902-68-4PF-04965842PF04965842PF 04965842JAKJanus kinaseInhibitorinhibitorinhibit

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