Tofacitinib, Free Base **

产品名称：Tofacitinib, Free Base
产品货号：LC  T-1377
产品规格：100 MG
This product was previously Cat. No. C-1377, CP-690550, and was also previously named Tasocitinib under the current Cat. No. T-1377.
Tofacitinib is a novel Janus kinase 3 (JAK3) inhibitor.  JAK3 is a critical cytoplasmic tyrosine kinase in the signaling pathways of multiple cytokines (interleukin (IL)-2, -7, -15 and -21) that are associated with various T cell functions.
Preclinical and clinical data strongly support that Tofacitinib, as an immunosuppressant, prevents organ transplant rejection and alleviates the symptoms of autoimmune diseases, such as rheumatoid arthritis (RA) and psoriasis.  West, K.  "CP-690550, a JAK3 inhibitor as an immunosuppressant for the treatment of rheumatoid arthritis, transplant rejection, psoriasis and other immune-mediated disorders."  Curr. Opin. Investig. Drugs 10:  491-504 (2009).
Tofacitinib showed greater antiproliferative and pro-apoptotic activity against murine multipotent factor-dependent cell Patersen-erythropoietin receptor (FDCP-EpoR) cells harboring JAK2(V617F) compared with JAK2(WT).  Manshouri, T., et al.  "The JAK kinase inhibitor CP-690,550 suppresses the growth of human polycythemia vera cells carrying the JAK2V617F mutation."  Cancer Sci. 99:  1265-1273 (2008).
JAK3 plays an important role in pulmonary eosinophilia in the allergic mouse model.  Tofacitinib, as a JAK3 inhibitor, represents a potential therapy for treatment of allergic conditions associated with airway eosinophilia including asthma and rhinitis.  Kudlacz, E., et al.  "The JAK-3 inhibitor CP-690550 is a potent anti-inflammatory agent in a murine model of pulmonary eosinophilia."  Eur. J. Pharmacol. 582:  154-161 (2008).
Tofacitinib was evaluated in murine collagen-induced (CIA) and rat adjuvant-induced (AA) models of rheumatoid arthritis (RA).  Tofacitinib dose-dependently reduced endpoints of disease in both RA models.  The compound also inhibited inflammatory cell influx and joint damage.  Milici, A.J., et al.  "Cartilage preservation by inhibition of Janus kinase 3 in two rodent models of rheumatoid arthritis."  Arthritis Res. Ther. 10:  R14 (2008).
Tofacitinib effectively blocked allograft vasculopathy in the rat model of aorta transplantation by inhibiting JAK3.  Rousvoal, G., et al.  "Janus kinase 3 inhibition with CP-690,550 prevents allograft vasculopathy."  Transpl. Int. 19:  1014-1021 (2006).
Combination treatment of Tofacitinib with mycophenolate mofetil (MMF) significantly improved allograft survival in nonhuman primates compared to treatment with MMF alone.  Borie, D.C., et al.  "Combined use of the JAK3 inhibitor CP-690,550 with mycophenolate mofetil to prevent kidney allograft rejection in nonhuman primates."  Transplantation 80:  1756-1764 (2005).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 100 mg/mL; soluble in ethanol at 100 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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