Fingolimod (FTY720) HCl

Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.

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Fingolimod (FTY720) HCl Chemical Structure

Fingolimod (FTY720) HCl Chemical Structure
Molecular Weight: 343.9

Validation & Quality Control

Customer Product Validation(3)

Quality Control & MSDS

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Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.
Targets S1P receptor [1]
(K562, NK cells )
IC50 0.033 nM
In vitro 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. [1] 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. [2]
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. [3]
Features

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines Immature DCs
Concentrations 10 nM
Incubation Time 4 hours
Method Immature DCs are left intact or are incubated with 2 μM S1P, 10 nM FTY720, 10 nM SEW2871 or the combinations of S1P with these drugs for 4 hours. As a control 1 μg/mL LPS is used. The cells are washed and incubated in a 96-well plate (v-bottom, 2 × 105 cells per well), washed again and resuspended in PBS buffer containing 0.1% sodium azide. They are labeled with 1 μg/mL FITC-conjugated mouse anti-human CD80, 1 μg/mL FITC-conjugated mouse anti-human CD83, 1 μg/mL FITC-conjugated mouse anti-human CD86, 1 μg/mL FITC-conjugated mouse anti-human HLA-class I, 1 μg/mL FITC-conjugated mouse anti-human HLA-DR, 1 μg/mL FITC-conjugated mouse anti-human HLA-E, or 1 μg/mL FITC-conjugated mouse IgG as a control. The cells are washed twice, and examined in the flow cytometer. Markers are set according to the isotype control FITC-conjugated mouse IgG. To stain NK cells with antibodies for various NK cell activating receptors, they are either left untreated or incubated with 2 μM S1P for 4 hours, washed and stained with 1 μg/mL PE-conjugated mouse anti-human NKp30 (CD337), 1 μg/mL PE-conjugated mouse anti-human NKp44 (CD336), 1 μg/mL PE-conjugated mouse anti-human NKG2D (CD314), or as a control 1 μg/mL PE-conjugated mouse IgG1, for 45 min at 4 °C. NK cells are also stained with 1 μg/mL FITC-conjugated anti-killer inhibitory receptor (KIR)/CD158 antibody which recognizes KIR2DL2, KIR2DL3, KIR2DS2 and KIR2DS4, and as a control with FITC-conjugated mouse IgG. The cells are washed twice, and examined in the flow cytometer. Markers are set according to the isotype control PE-conjugated or FITC-conjugated mouse IgG.

Animal Study: [3]

Animal Models NOD/SCIDγc−/− mice bearing ALL cells.
Formulation 2% ethanol or saline
Dosages 5 mg/kg/day, 10 mg/kg/day
Administration Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rolin J, et al. Cancer Immunol Immunother. 2010, 59(4), 575-586.

[2] Liu Y, et al. Int J Mol Med. 2012, 30(1), 211-219.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-05-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02373098 Not yet recruiting Relapsing Remitting Multiple Sclerosis Novartis Pharmaceuticals|Novartis March 2015 Phase 4
NCT02373098 Not yet recruiting Relapsing Remitting Multiple Sclerosis Novartis Pharmaceuticals|Novartis March 2015 Phase 4
NCT02342704 Recruiting Relapsing-Remitting Multiple Sclerosis Biogen Idec November 2014 Phase 4
NCT02342704 Recruiting Relapsing-Remitting Multiple Sclerosis Biogen Idec November 2014 Phase 4
NCT02232061 Recruiting Multiple Sclerosis Novartis Pharmaceuticals|Novartis September 2014 Phase 4

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Chemical Information

Download Fingolimod (FTY720) HCl SDF
Molecular Weight (MW) 343.9
Formula

C19H33NO2.HCl

CAS No. 162359-56-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * 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
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-(4-octylphenethyl)-2-aminopropane-1,3-diol hydrochloride

Research Area

Customer Product Validation (3)


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Rating
Source Blood 2012 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck
Method Survival assay
Cell Lines SCID mice
Concentrations 2ug/g
Incubation Time 50 day
Results Fingolimod efficiently blocked rejection of both MOPC315 myeloma and F9 B-cell lymphoma by TCR-transgenic mice.

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Rating
Source Blood 2012 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck
Method
Cell Lines SCID mice
Concentrations 1ug/g
Incubation Time 8 day
Results fingolimod blocks immunosurveillance of B-cell cancers by suppressing migration of tumor-specific Th1 cells from lymph nodes to the incipient tumor site, thereby preventing Th1-mediated activation of tumoricidal macrophages.

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Rating
Source Mol Med 2011 17, 717- 725 . Fingolimod (FTY720) HCl purchased from Selleck
Method In vivo study
Cell Lines C57BL/6 WT animals
Concentrations 0.3 mg/kg
Incubation Time 9-15 day
Results Plasma sICAM-1, a marker of endothelialactivation (33), was decreased inFTY720-treated mice compared with untreatedmice (Figure 3A). Elevated levelsin infected but untreated mice were decreasedsignificantly in all animalstreated with FTY720 (P < 0.0001). Conversely,plasma Ang1, a marker of endotheliumquiescence and stability, wasincreased in mice treated with FTY720prophylactically compared with untreatedanimals (P = 0.02, Figure 3B).Studies observing Evans blue stainingof the brain demonstrated that FTY720treatment improved BBB integrity inECM.

Product Use Citation (21)

Tech Support & FAQs

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