Abrocitinib (PF-04965842) (Synonyms: PF-04965842) |
| Catalog No.GC32023 |
아브로시티닙(PF-04965842)(PF-04965842)은 강력한 경구 활성 및 선택적 JAK1 억제제이며 JAK1 및 JAK2에 대해 각각 IC50이 29 및 803nM입니다.
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Cas No.: 1622902-68-4
Sample solution is provided at 25 µL, 10mM.
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Abrocitinib (PF-04965842) is a potent, oral 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[1].
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[1].
[1]. Vazquez ML, et al. Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. J Med Chem. 2018 Feb 8;61(3):1130-1152.
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