PF-06700841

Catalog No.S8804 Synonyms: PF-841

PF-06700841 Chemical Structure

Molecular Weight(MW): 389.40

PF-06700841 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.

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Biological Activity

Description PF-06700841 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

Animal Research:

[1]

+ Expand
  • Animal Models: Rat adjuvant induced arthritis model (8−10 weeks old female Lewis rats)
  • Formulation: 2% Tween 80/0.5% methylcellulose/deionized H2O
  • Dosages: 3, 10, or 30 mg/kg/day
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (200.3 mM)
Ethanol 78 mg/mL (200.3 mM)
Water 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.

Chemical Information

Molecular Weight 389.40
Formula

C18H21F2N7O

CAS No. 1883299-62-4
Storage powder
in solvent
Synonyms PF-841

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID