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PF-06700841 tosylate

Cat. No. M9853
PF-06700841 tosylate Structure
Synonym:

CS-2860; Brepocitinib

Size Price Availability Quantity
25mg USD 312.3  USD347 In stock
50mg USD 535.5  USD595 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PF-06700841 (Brepocitinib) is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively. PF-06700841 (Brepocitinib) inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50 of 577 nM). PF-06700841 also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC50s of 238 and 204 nM, respectively).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 561.60
Formula C25H29F2N7O4S
CAS Number 2140301-96-6
Purity >99%
Solubility DMSO 57 mg/mL
Storage at -20°C
References

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)
Andrew Fensome, et al. J Med Chem. 2018 Oct 11;61(19):8597-8612. PMID: 30113844.

The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF-06700841) in Healthy Subjects and Patients With Plaque Psoriasis
Christopher Banfield, et al. J Clin Pharmacol. 2018 Apr;58(4):434-447. PMID: 29266308.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-06700841 tosylate, CS-2860; Brepocitinib supplier, JAK, inhibitors

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