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Brepocitinib P-Tosylate

Cat. No. M9853
Brepocitinib P-Tosylate Structure

CS-2860; Brepocitinib;PF-06700841 P-Tosylate

Size Price Availability Quantity
10mg USD 120  USD120 In stock
25mg USD 272  USD272 In stock
50mg USD 495  USD495 In stock
100mg USD 840  USD840 In stock
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Quality Control & Documentation
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).

Chemical Information
Molecular Weight 561.60
Formula C25H29F2N7O4S
CAS Number 2140301-96-6
Solubility (25°C) DMSO 57 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.


[1] Andrew Fensome, et al. J Med Chem. 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)

[2] Christopher Banfield, et al. J Clin Pharmacol. The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF-06700841) in Healthy Subjects and Patients With Plaque Psoriasis

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Keywords: Brepocitinib P-Tosylate, CS-2860; Brepocitinib;PF-06700841 P-Tosylate supplier, JAK, inhibitors, activators

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