托法替尼Tofacitinib477600-75-2上海惠诚

Tofacitinib (477600-75-2) is a potent pan-JAK inhibitor, IC50s=1, 20 and 112 nM for JAK3, JAK2 and JAK1 respectively.1 Displays potent antiinflammatory2 and immunosuppressant3 activity. Promotes a white-to-brown metabolic conversion in human adipoctes.4 In therapeutic use for rheumatoid arthritis.5

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References/Citations
1) Jiang et al. (2008), Examining the chirality, confirmation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitril (CP-690,550); J. Mol. Chem., 51 8012
2) Cutolo and Meroni (2013), Clinical utility of the oral JAK inhibitor tofacitinib in the treatment of rheumatoid arthritis; J. Inflamm. Res., 6 129
3) Martina et al. (2016), Inhiition of JAK3 and PKC via Immunosuppressive Drugs Tofacitinib and Sotrastaurin Inhibits Proliferation of Human B Lymphocytes In Vitro; Transplant. Proc., 48 3046
4) Moisan et al. (2015), White-to-brown metabolic conversion of human adipocytes by JAK inhibition; Nat. Cell Biol., 17 57
5) Dowty et al. (2014), Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis; J. Pharmacol. Exp. Ther., 348 165