ChemicalBook > CAS DataBase List > PF-06700841 tosylate

PF-06700841 tosylate

Product Name
PF-06700841 tosylate
CAS No.
1883299-62-4
Chemical Name
PF-06700841 tosylate
Synonyms
PF841;PF 841;PF-841;CS-2861;PF6700841;PF 6700841;PF-6700841;PF-06700841 tosylate;Brepocitinib (PF-06700841);inhibit,Janus kinase,PF06700841,JAK,Brepocitinib,Inhibitor,PF 06700841
CBNumber
CB94674167
Molecular Formula
C18H21F2N7O
Formula Weight
389.4
MOL File
1883299-62-4.mol
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PF-06700841 tosylate Property

Boiling point:
637.1±65.0 °C(Predicted)
Density 
1.63±0.1 g/cm3(Predicted)
storage temp. 
room temp
solubility 
DMSO: 78 mg/mL (200.31 mM);Ethanol: 78 mg/mL (200.31 mM)
form 
powder
pka
7.28±0.10(Predicted)
color 
white to beige
Water Solubility 
Water: Insoluble
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0345
Product name
PF-06700841 tosylate salt
Purity
≥98% (HPLC)
Packaging
5mg
Price
$114
Updated
2024/03/01
Biorbyt Ltd
Product number
orb573132
Product name
PF-06700841 tosylate
Purity
>98%
Packaging
100mg
Price
$1283.5
Updated
2021/12/16
Biorbyt Ltd
Product number
orb573132
Product name
PF-06700841 tosylate
Purity
>98%
Packaging
250mg
Price
$2245.7
Updated
2021/12/16
Biorbyt Ltd
Product number
orb573132
Product name
PF-06700841 tosylate
Purity
>98%
Packaging
1g
Price
$4766.8
Updated
2021/12/16
DC Chemicals
Product number
DC12489
Product name
PF-06700841freebase
Purity
>98%
Packaging
1g
Price
$3200
Updated
2021/12/16
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PF-06700841 tosylate Chemical Properties,Usage,Production

Chemical Properties

The p-toluenesulfonic acid salt of brepocitinib exhibits good aqueous solubility (4.84 mg/mL at pH 7.64; >7 mg/mL in simulated gastric fluids). This compound also displayed high passive membrane permeability (mean PAPP = 18.8 × 10?6 cm/s as determined using Ralph Russ canine kidney cells (RRCK)).

Characteristics

Class: non-receptor tyrosine kinase
Treatment: immunological disorders
Other name: PF-06700841; Brepocitinib
Elimination half-life = 3.8–7.5 h
Protein binding = 39%

Uses

PF-06700841 tosylate salt has been used as an inhibitor of Janus kinase1 (JAK1) to study its therapeutic effect on the adjuvant induced arthritis (AIA) rat model. It has also been used as an inhibitor of interferon-α/β receptor alpha chain (IFNAR1) signaling adaptor tyrosine kinase (2TYK2) in mice.

Biochem/physiol Actions

PF-06700841 prevents IL-23 (interleukin 23) signaling through TYK2 (Tyrosine-protein kinase 2)/JAK1 (Janus kinase 1) inhibition.

Pharmacokinetics

The high oral bioavailability of brepocitinib obtained from rats (83%) is consistent with its high passive permeability and good solubility. The elimination half-life of brepocitinib ranged from 3.8 to 7.5 h after a single oral dose and from 4.9 to 10.7 h after multiple-dose administration. It was eliminated from the body by CYP450-mediated hepatic metabolism (84%) (mainly via CYP3A4) and renal clearance (16%). Oxidation of the N-methyl pyrazole (2) is the major metabolic pathway, followed by N-demethylation (3) and N-dealkylation with loss of pyrazole (4).

PF-06700841 tosylate Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-06700841 tosylate Suppliers

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1883299-62-4, PF-06700841 tosylateRelated Search:


  • PF-06700841 tosylate
  • ((S)-2,2-difluorocyclopropyl)(3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone
  • PF 6700841
  • PF-06700841; PF 06700841; PF06700841; PF-6700841; PF 6700841; PF6700841; PF-06700841 TOSYLATE SALT
  • PF6700841
  • PF-6700841
  • CS-2861
  • ((S)-2,2-difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone
  • Methanone, [(1S)-2,2-difluorocyclopropyl][3-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-3,8-diazabicyclo[3.2.1]oct-8-yl]-
  • Brepocitinib (PF-06700841)
  • inhibit,Janus kinase,PF06700841,JAK,Brepocitinib,Inhibitor,PF 06700841
  • PF 841
  • PF841
  • PF-841
  • 1883299-62-4
  • C18H21F2N7O
  • api
  • APIS