Brepocitinib (PF-06700841)

Catalog No.S8804 Batch:S880401

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Technical Data

Formula

C18H21F2N7O
Molecular Weight 389.40 CAS No. 1883299-62-4
Solubility (25°C)* In vitro DMSO 78 mg/mL (200.3 mM)
Ethanol 78 mg/mL (200.3 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.97mg/ml Taking the 1 mL working solution as an example, add 50 μL of 19.4 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.9mg/ml Taking the 1 mL working solution as an example, add 50 μL of 78 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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 Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
Targets
JAK1 [1]
(Cell-free assay)		 Tyk2 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)
17 nM 23 nM 77 nM
In vivo

The pharmacokinetics of PF-06700841 are studied in Sprague−Dawley rats following intravenous and oral administration (1 and 3 mg/kg respectively) of the tosylate salt, where the compound shows a plasma clearance of 31 mL/min/kg, a volume of distribution of 2.0 L/kg, and oral bioavailability of 83%. Following the 3 mg/kg oral dose, the Cmax is 774 ng/mL and the AUC∞ is 1340 ng·h/mL. The high oral bioavailability indicates high absorption from the gut, consistent with its in vitro passive permeability properties and high solubility[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Rat adjuvant induced arthritis model (8−10 weeks old female Lewis rats)

  • Dosages

    3, 10, or 30 mg/kg/day

  • Administration

    oral administration

Selleck's Brepocitinib (PF-06700841) has been cited by 1 publication

Oncogenic KIT Modulates Type I IFN-Mediated Antitumor Immunity in GIST [ Cancer Immunol Res, 2021, 9-5:542-553] PubMed: 33648985

RETURN POLICY
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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.