產(chǎn)品目錄

規(guī)格	1 mg
CAS	N/A
別名	N/A
化學(xué)名	N/A
分子式	C16H17D3N6O ? C6H8O7
分子量	507.5
溶解度	DMSO: soluble,Water: soluble
儲存條件	-20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)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).1 It 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.2 Tofacitinib 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)

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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