PF-06700841 tosylate

PF-06700841 tosylate Structure
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
Molecular Weight:
389.4
MOL File:
1883299-62-4.mol
Modify Date:
2024/5/28 11:51:27

PF-06700841 tosylate Properties

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

PF-06700841 tosylate price More Price(1)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) PZ0345 PF-06700841 tosylate salt ≥98% (HPLC) 1883299-62-4 5MG ₹10230 2022-06-14 Buy
Product number Packaging Price Buy
PZ0345 5MG ₹10230 Buy

PF-06700841 tosylate Chemical Properties,Uses,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

PF-06700841 tosylate Preparation Products And Raw materials

Raw materials

Preparation Products

PF-06700841 tosylate Suppliers

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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