Basic information Safety Supplier Related

PF-06700841-TsOH

Basic information Safety Supplier Related

PF-06700841-TsOH Basic information

Product Name:
PF-06700841-TsOH
Synonyms:
  • PF-06700841-TsOH
  • PF-06700841 free base
  • CS-2860
  • PF-06700841 P-TOSYLATE
  • Brepocitinib tosylate
  • Brepocitinib (P-Tosylate)
  • Janus kinase,JAK,Brepocitinib P-Tosylate,inhibit,Brepocitinib PTosylate,Inhibitor,Brepocitinib P Tosylate
  • PF 06700841-15
CAS:
2140301-96-6
MF:
C25H29F2N7O4S
MW:
561.61
Product Categories:
  • API
Mol File:
2140301-96-6.mol
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PF-06700841-TsOH Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:20): 50μg/ml; Ethanol: slightly soluble
form 
A crystalline solid
color 
White to off-white
InChIKey
FAKGOYNHHHOTEN-QYGWXNHUNA-N
SMILES
S(C1C=CC(C)=CC=1)(O)(=O)=O.C([C@@H]1CC1(F)F)(N1C2CCC1CN(C1C=CN=C(NC3=CN(C)N=C3)N=1)C2)=O |&1:12,r|
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PF-06700841-TsOH Usage And Synthesis

Uses

Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively[1].

in vivo

Brepocitinib (Compound 23; 3-30 mg/kg; oral administration; 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 Brepocitinib 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[1].

Animal Model:Female Lewis rats with induced arthritis[1]
Dosage:3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration:Oral administration; for 7 consecutive days
Result:Increased in paw volume was significantly lower and dose-dependent.

IC 50

JAK1: 17 nM (IC50); JAK2: 77 nM (IC50); JAK3: 6.9 μM (IC50)

References

[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-06700 DOI:10.1021/acs.jmedchem.8b00917

PF-06700841-TsOHSupplier

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PF-06700841-TsOH(2140301-96-6)Related Product Information