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Brepocitinib

Catalog No. TQ0010   CAS 1883299-62-4
Synonyms: PF-06700841

Brepocitinib is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). Brepocitinib also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).

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Brepocitinib, CAS 1883299-62-4
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Purity 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Brepocitinib is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). Brepocitinib also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
In vitro PF-06700841 inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood IC50s: 65/120 nM). PF-06700841 inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (IC50s: 238/204 nM). PF-06700841 also has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50: 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50: 641 nM). PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50: 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 (IC50s: 305 nM/86 nM).
In vivo PF-06700841 (3-30 mg/kg; p.o; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with PF-06700841 at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM.
Synonyms PF-06700841
Molecular Weight 389.4
Formula C18H21F2N7O
CAS No. 1883299-62-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 75 mg/mL (192.60 mM)

H2O: Insoluble

H2O: Insoluble

Ethanol: 75 mg/mL (192.60 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Fensome A, et al. Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). J Med Chem. 2018 Oct 11;61(19):8597-8612.

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