Description
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.
Product information
CAS Number: 1622902-68-4
Molecular Weight: 323.41
Formula: C14H21N5O2S
Chemical Name: N-[(1s,3s)-3-[methyl({7H-pyrrolo[2,3-d]pyrimidin-4-yl})amino]cyclobutyl]propane-1-sulfonamide
Smiles: CCCS(=O)(=O)N[C@@H]1C[C@@H](C1)N(C)C1N=CN=C2NC=CC=12
InChiKey: IUEWXNHSKRWHDY-PHIMTYICSA-N
InChi: InChI=1S/C14H21N5O2S/c1-3-6-22(20,21)18-10-7-11(8-10)19(2)14-12-4-5-15-13(12)16-9-17-14/h4-5,9-11,18H,3,6-8H2,1-2H3,(H,15,16,17)/t10-,11+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (386.51 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively.
In Vivo:
Abrocitinib (Compound 25; 5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling in rat adjuvant-induced arthritis model.
Products are for research use only. Not for human use.
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