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Tofacitinib-d3(citrate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tofacitinib-d3(citrate)图片
包装:1mg
市场价:8316元

产品介绍
An internal standard for the quantification of tofacitinib
别名Tasocitinib-d3 citrate; CP-690550-d3 citrate
Canonical SMILESO=C(CC#N)N1CC[C@@H](C)[C@@H](N(C([2H])([2H])[2H])C2=NC=NC3=C2C=CN3)C1.OC(CC(O)=O)(C(O)=O)CC(O)=O
分子式C16H17D3N6O • C6H8O7
分子量507.5
溶解度DMSO: soluble,Water: soluble
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Tofacitinib-d3(citrate) is intended for use as an internal standard for the quantification of tofacitinib by GC- or LC-MS. Tofacitinib is a potent, cell-permeable inhibitor of all JAK isoforms (IC50s = 6.1, 12, and 8 nM for JAK1, JAK2, and JAK3, respectively).1It is selective for JAK1-3 over ROCK-2 and Lck (IC50s = 3,400 and 3,870 nM, respectively) as well as 28 additional kinases in enzyme assays (IC50s = >10,000 nM). It inhibits IL-2-mediated phosphorylation of JAK3 and STAT5 when used at a concentration of 30 ng/ml.2Tofacitinib prevents rejection and prolongs survival in murine and cynomolgus monkey models of heterotopic heart and kidney transplantation, respectively. Formulations containing tofacitinib have been used in the prevention of organ allograft rejection as well as in the treatment of the inflammatory or autoimmune components of a host of diseases, including rheumatoid arthritis and ulcerative colitis.2,3,4,5

1.Haan, C., Rolvering, C., Raulf, F., et al.Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptorsChem. Biol.18(3)314-323(2011) 2.Changelian, P.S., Flanagan, M.E., Ball, D.J., et al.Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitorScience302(5646)875-878(2003) 3.Flanagan, M.E., Blumenkopf, T.A., Brissette, W.H., et al.Discovery of CP-690,550: A potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejectionJ. Med. Chem.53(24)8468-8484(2010) 4.Cutolo, M.The kinase inhibitor tofacitinib in patients with rheumatoid arthritis: Latest findings and clinical potentialTher. Adv. Musculoskelet. Dis.5(1)3-11(2013) 5.Sandborn, W.J., Ghosh, S., Panes, J., et al.Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitisN. Engl. J. Med.367(7)616-624(2012)