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 37 Publications
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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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03345940||Recruiting||Drug: Fingolimod|Drug: Dimethyl Fumarate||Relapsing Remitting Multiple Sclerosis||Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta|Patient-Centered Outcomes Research Institute|Universita degli Studi di Genova||April 30 2017||Phase 4|
|NCT02575365||Terminated||Drug: 05 mg Fingolimod||Cognition|Brain Volume Loss||Novartis Pharmaceuticals|Novartis||February 16 2016||Phase 4|
|NCT02490930||Completed||Drug: Fingolimod||Glioblastoma|Anaplastic Astrocytoma||Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins||July 2015||Early Phase 1|
|NCT01981161||Unknown status||Procedure: biological samples and clinical data||Multiple Sclerosis||University Hospital Toulouse|European Commission||November 2013||--|
|NCT01791192||Withdrawn||Drug: FTY720|Drug: Oral Corticosteroid||Acute Noninfectious Posterior Intermediate or Pan Uveitis||Novartis Pharmaceuticals|Novartis||November 2013||Phase 2|
|NCT01757691||Terminated||Drug: Fingolimod 0.5mg/daily|Drug: Placebo||Acute Demylelinating Optic Neuritis||Novartis Pharmaceuticals|Novartis||August 2013||Phase 2|
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