PF-06700841-TsOH
- Product Name
- PF-06700841-TsOH
- CAS No.
- 2140301-96-6
- Chemical Name
- PF-06700841-TsOH
- Synonyms
- CS-2860;PF 06700841-15;PF-06700841-TsOH;PF-06700841 free base;Brepocitinib tosylate;PF-06700841 P-TOSYLATE;Brepocitinib (P-Tosylate);Brepocitinib P-Tosylate, 10 mM in DMSO;Janus kinase,JAK,Brepocitinib P-Tosylate,inhibit,Brepocitinib PTosylate,Inhibitor,Brepocitinib P 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 4-methylbenzenesulfonate
- CBNumber
- CB94675331
- Molecular Formula
- C25H29F2N7O4S
- Formula Weight
- 561.61
- MOL File
- 2140301-96-6.mol
PF-06700841-TsOH Property
- 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|
N-Bromosuccinimide Price
- Product number
- 26125
- Product name
- PF-06700841 (tosylate)
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 26125
- Product name
- PF-06700841 (tosylate)
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
- Product number
- 26125
- Product name
- PF-06700841 (tosylate)
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $343
- Updated
- 2024/03/01
- Product number
- 26125
- Product name
- PF-06700841 (tosylate)
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- CS-0066286
- Product name
- PF-06700841(P-Tosylate)
- Purity
- 99.66%
- Packaging
- 10mg
- Price
- $140
- Updated
- 2021/12/16
PF-06700841-TsOH Chemical Properties,Usage,Production
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-TsOH Preparation Products And Raw materials
Raw materials
Preparation Products
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