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
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
N-Bromosuccinimide Price
- Product number
- PZ0345
- Product name
- PF-06700841 tosylate salt
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $114
- Updated
- 2024/03/01
- Product number
- orb573132
- Product name
- PF-06700841 tosylate
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1283.5
- Updated
- 2021/12/16
- Product number
- orb573132
- Product name
- PF-06700841 tosylate
- Purity
- >98%
- Packaging
- 250mg
- Price
- $2245.7
- Updated
- 2021/12/16
- Product number
- orb573132
- Product name
- PF-06700841 tosylate
- Purity
- >98%
- Packaging
- 1g
- Price
- $4766.8
- Updated
- 2021/12/16
- Product number
- CD31005024
- Product name
- 4-[(1R,5S)-8-[(1S)-2,2-difluorocyclopropanecarbonyl]-3,8-diazabicyclo[3.2.1]octan-3-yl]-N-(1-methyl-1H-pyrazol-4-yl)pyrimidin-2-amine
- Purity
- 98%
- Packaging
- 25mg
- Price
- $480
- Updated
- 2021/12/16
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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