Fingolimod(FTY720) (Synonyms: Gilenia; FTY 720; FTY-720) |
Catalog No.GC14807 |
Fingolimod (FTY720) HCl (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 162359-56-0
Sample solution is provided at 25 µL, 10mM.
Fingolimod (FTY720), an immunosuppressant agent, usually used in the treatment of multiple sclerosis, also has anticancer actions and can act as an HDACi (Histone deacetylase inhibitors)[1].
In vitro, Fingolimod at 7.5 or 10 µM, induced a significant reduction in cell viability in D283 and DAOY cultures, also led to a significant increase in the levels of acetylated H3[1]. In vitro, Fingolimod showed cytotoxic antiproliferative effects against androgen-dependent and -independent prostate cancer cells with IC50 ranging from 3.0 ± 0.3 to 6.8 ± 1.7 µM[2]. Jurkat T-lymphocytes exposure to Fingolimod suppressed the amplitude of delayed-rectifier K+ current (IK(DR)) in a time- and concentration-dependent manner with an IC50 value of 1.51 µM[3]. Fingolimod reduced the proliferation and viability of Ph(+) and Ph(-) ALL cell lines and patient samples with IC 50 values for viability between 5.3 to 7.9 µM[4]. Fingolimod differentially suppressed the viability of the OSCC cell lines SCC4, SCC25, and SCC2095 with IC50 values of 6.1, 6.3, and 4.5 µM, respectively[5].
In vivo, E13 C57BL/6 wildtype mice were treated with 1 mg/kg significantly increased the survival of DCX+ neurons in the DG (dentate gyrus) and the SVZ (the subventricular zone) 4 weeks after irradiation as well as a slight increase of proliferating cells[6]. In vivo, 5xFAD mice were treated with 1 mg/kg/day fingolimod decreased both peripheral blood lymphocyte counts and brain Aβ levels, but treated with 0.03 mg/kg/day improved memory, decreased activation of brain microglia and astrocytes, and restored hippocampal levels of GABA and glycerophosphocholine with no effect on circulating lymphocyte counts[7]. In vivo, C57BL/6JOlaHsd mice were treated with 0.5 mg/kg fingolimod increased lesion size (stroke) but decreased ipsilateral brain atrophy in younger mice, without an effect on behavioural outcomes[8].
References:
[1] Perla AS, et al. Fingolimod (Fingolimod) reduces viability and survival and increases histone H3 acetylation in medulloblastoma cells. Pediatr Hematol Oncol. 2020 Mar;37(2):170-175.
[2] Allam RM, et al. Fingolimod interrupts the cross talk between estrogen metabolism and sphingolipid metabolism within prostate cancer cells. Toxicol Lett. 2018 Jul;291:77-85.
[3] Chang WT, et al. Actions of Fingolimod (Fingolimod), a Sphingosine-1-Phosphate Receptor Modulator, on Delayed-Rectifier K+ Current and Intermediate-Conductance Ca2+-Activated K+ Channel in Jurkat T-Lymphocytes. Molecules. 2020 Oct 2;25(19):4525.
[4] Wallington-Beddoe CT, et al. Fingolimod produces caspase-independent cell death of acute lymphoblastic leukemia cells. Autophagy. 2011 Jul;7(7):707-15.
[5] Bai LY, et al. Fingolimod Induces Autophagy-Associated Apoptosis in Human Oral Squamous Carcinoma Cells, in Part, through a Reactive Oxygen Species/Mcl-1-Dependent Mechanism. Sci Rep. 2017 Jul 17;7(1):5600.
[6] Metzdorf J, et al. Fingolimod for Irradiation-Induced Neurodegeneration. Front Neurosci. 2019 Jul 9;13:699.
[7] Carreras I, et al. Dual dose-dependent effects of fingolimod in a mouse model of Alzheimer's disease. Sci Rep. 2019 Jul 29;9(1):10972.
[8] Diaz Diaz AC, et al. Preclinical Evaluation of Fingolimod in Rodent Models of Stroke With Age or Atherosclerosis as Comorbidities. Front Pharmacol. 2022 Jul 13;13:920449.
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