• Catalog Number:

  E1KS5002

• Amount:

  100mg1​ PHYSICAL AND CHEMICAL PROPERTIES

2​ Biological Activity FTY720(Fingolimod) is a potent sphingosine-1-phosphate (S1P) receptors agonist with IC50 of 0.137, 10.98 nM for (S)- and (R)- FTY720-phosphate, respectively and reverses the effects of BCR-ABL kinase. It is a novel immunomodulating agent and can sequester lymphocytes in lymph nodes, preventing them from moving to the central nervous system for auto-immune responses in multiple sclerosis and was originally proposed as a anti-rejection medication indicated post-transplantation. [1] It can be phosphorylated by sphingosine kinase and prevents disease in a mouse model of many leukemias caused by BCR-ABL. It does not directly target the BCR-ABL kinase, but instead activates phosphatase 2A (PP2A) which is a tumor suppressor that is inactivated by BCR-ABL. [2] FTY720(Fingolimod) also mediated antitumor effects in hepatocellular carcinoma (HCC) cells by activating PKC . The three HCC cell lines examined, Hep3B, Huh7, and PLC5, exhibited differential susceptibility to FTY720-mediated suppression of cell viability, with IC50 values of 4.5, 6.3, and 11 μM, respectively. [3] 3​ References: [1] http://en.wikipedia.org/wiki/Fingolimod [2] Neviani P et al. J Clin Invest. 2007 Sep;117(9):2408-21. [3] Hung JH et al. Cancer Res. 2008 Feb 15;68(4):1204-12. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.