Fingolimod (FTY720) HCl
Molecular Weight(MW): 343.9
Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.
Cited by 23 Publications
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Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6 105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8).
Blood 2012 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck.
Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. Id-specific TCR-transgenic and nontransgenic SCID mice were inoculated subcutaneously with 105 MOPC315 myeloma cells embedded in Matrigel.9 TCR-transgenic SCID mice were treated daily with fingolimod (1ug/g bodyweight) or with vehicle only (n=8-10). SCID mice were left untreated (n =2). At day 8, draining lymph nodes and Matrigel plugs were dissected and analyzed by flow cytometry.9 (D) CD69 expression on gated Id-specific CD4 T cells in draining lymph nodes of representative TCR-transgenic SCID mice treated with vehicle only (top) or fingolimod (bottom). Dotted lines indicate an isotype-matched control antibody. (E) Number of Id-specific T cells per Matrigel plug (mean SEM). (F) Expression of the activation marker MHC class II on Matrigel-infiltrating CD11b macrophages (geometric mean SEM). P values were calculated with the log-rank test (A-C) and the t test (E-F). ns indicates not significant.
Blood 2012 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck.
FTY720 treatment of ECM decreases lymphocyte numbers and granzyme A mRNA in the brain. (A) Relative CD8+ and (B) CD4+ T-cell numbers isolated from the brains of mice infected for 6 d. Numbers were decreased in animals treated with FTY720 1 d before infection and 1 d p.i. (CD4+: P < 0.5 and P < 0.001, CD8+: P < 0.5 and P < 0.01 respectively, KW and DMC, two pooled IE, n ≥ 4/group/IE) (C) GZMA mRNA levels were decreased in the brains of FTY720-treated animals compared with control animals: for (FTY720 [–1], P < 0.05, FTY720 [+1] P > 0.05 and FTY720 [+3], P < 0.01; KW and DMC, two pooled IE, n ≥ 3/group/IE).
Mol Med 2011 17, 717- 725 . Fingolimod (FTY720) HCl purchased from Selleck.
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|Description||Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.|
The inhibitory effect of S1P is revered by various concentrations of FTY720, with IC50 effect of 173 nM. In addition, FTY720 (10 nM) alone exerts no effect on the expression of co-stimulatory molecules. FTY720 reverses the increased expression of HLA-I induced by S1P for both the percentages of cells and the MFI, upon comparing the effect of S1P to the effect of combining S1P with FTY720.  Medium and high-dose FTY720-P also enhances the levels of TGF-β1. TGF-β1 and Foxp3 mRNA expression are upregulated in the high-dose FTY720-P group. The proliferation of effector T cells is suppressed significantly in the medium and high-dose FTY720-P group at a Treg/Teff cell ratio of 1:1. At a ratio of 1:1, the proliferation of effector T cells is also suppressed in the high-dose FTY720 group. 
|In vivo||FTY720 is effective in Ph+ but not Ph- ALL xenografts using an early disease model. FTY720 produces a significant reduction in disease burden in the Ph+ ALL xenografts using an early disease model. Ph+ human ALL xenografts responds to FTY720 with an 80 % reduction in overall disease if treatment has been initiated early on. In contrast, treatment of mice with FTY720 does not result in reduced leukemia compared to controls using four separate human Ph- ALL xenografts. |
|In vitro||DMSO||69 mg/mL (200.63 mM)|
|Water||69 mg/mL (200.63 mM)|
|Ethanol||69 mg/mL (200.63 mM)|
|In vivo||Saline||20 mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02575365||Recruiting||Cognition,|Brain Volume Loss||Novartis Pharmaceuticals|Novartis||February 2016||Phase 4|
|NCT02632591||Completed||Multiple Sclerosis|Autoimmune Disease|Disseminated or Multiple Sclerosis Nos|Multiple Sclerosis, Acute Relapsing|Multiple Sclerosis, Primary Progressive|Multiple Sclerosis, Chronic Progressive||Università Popolare Homo & Natura||August 2015||Phase 1|
|NCT02490930||Recruiting||Glioblastoma|Anaplastic Astrocytoma||Sidney Kimmel Comprehensive Cancer Center||July 2015||Phase 0|
|NCT02373098||Recruiting||Relapsing Remitting Multiple Sclerosis||Novartis Pharmaceuticals|Novartis||March 2015||Phase 4|
|NCT02342704||Terminated||Relapsing-Remitting Multiple Sclerosis||Biogen||November 2014||Phase 4|
|NCT02232061||Recruiting||Multiple Sclerosis||Novartis Pharmaceuticals|Novartis||September 2014||Phase 4|
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