Abrocitinib (PF-04965842)

Catalog No.S8765 Batch:S876501

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Technical Data

Formula

C14H21N5O2S
Molecular Weight 323.41 CAS No. 1622902-68-4
Solubility (25°C)* In vitro DMSO 65 mg/mL (200.98 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
3.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Abrocitinib (PF-04965842) is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.
Targets
JAK1 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 TYK2 [1]
(Cell-free assay)
29 nM 803 nM 1.253 μM
In vitro

Abrocitinib (PF-04965842) is a potent JAK inhibitor with IC50 of 29 and 803 nM for JAK1 and JAK2, respectively.
In vivo

Physicochemical properties and pharmacokinetic parameters of PF-04965842 are examined in rats following doses of 1 mg/kg iv or 3 mg/kg po. Clearance of PF-04965842 is low relative to total liver blood flow (CL = 26.6 mL/min/kg). Vdss = 1.04 L/kg. T1/2 = 1.1 h. The oral availability of PF-04965842 is 95.6%. PF-04965842 demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Female Lewis rats (8−10 weeks old)

  • Dosages

    50, 15, 5 and 0.5 mg/kg

  • Administration

    via oral gavage

Selleck's Abrocitinib (PF-04965842) has been cited by 7 publications

Spatial proteomics identifies JAKi as treatment for a lethal skin disease [ Nature, 2024, ] PubMed: 39415009
Novel JAK Inhibitors to Reduce Graft-Versus-Host Disease after Allogeneic Hematopoietic Cell Transplantation in a Preclinical Mouse Model [ Molecules, 2024, 29(8)1801] PubMed: 38675621
Model of Chronic Itch in Aged Mice: Beneficial Effects of Drugs Affecting Descending Modulatory Systems [ Acta Derm Venereol, 2024, 104:adv39950] PubMed: 38751178
Abrocitinib Attenuates Microglia-Mediated Neuroinflammation after Traumatic Brain Injury via Inhibiting the JAK1/STAT1/NF-κB Pathway [ Cells, 2022, 11(22)3588] PubMed: 36429017
Adipose Tissue-Derived Mesenchymal Stem Cells Suppress Growth of Huh7 Hepatocellular Carcinoma Cells via Interferon (IFN)-β-Mediated JAK/STAT1 Pathway in vitro. [ Int J Med Sci, 2020, 18;17(5):609-619] PubMed: 32210710
Bortezomib-inducible long non-coding RNA myocardial infarction associated transcript is an oncogene in multiple myeloma that suppresses miR-29b. [ Cell Death Dis, 2019, 10(4):319] PubMed: 30967527
Roseburia intestinalis-derived flagellin is a negative regulator of intestinal inflammation [ Biochem Biophys Res Commun, 2018, 501(3):791-799] PubMed: 29772233

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.