Fingolimod (FTY720) HCl

For research use only.

Catalog No.S5002

78 publications

Fingolimod (FTY720) HCl Chemical Structure

CAS No. 162359-56-0

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

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Selleck's Fingolimod (FTY720) HCl has been cited by 78 publications

Purity & Quality Control

Choose Selective S1P Receptor Inhibitors

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 )
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U2OS cells NWDHV2pFTnWwY4Tpc44h[XO|YYm= MXLB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGOxVFEhemWlZYD0c5Ih\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiY3:t[ZhxemW|c3nu[{BmT0[SIHHzd4V{e2WmIHHzJJJm[2WydH;yJIlvfGW{bnHsbZpifGmxbjDpcpRwKGO7dH;wcIF{dSC3c3nu[{BJd2WlaIP0JIR6\SC|dHHpcolv\yxiRVO1NF0xNjByMjFOwG0v NXrQS3R5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxNFQyPDRpPkKyNVA1OTR2PD;hQi=>
human PC3 cells M{HWb2N6fG:2b4jpZ:Kh[XO|YYm= M4XOUlczKGh? M1:xNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bi\nSncjC3NkBpenNiYomgeol1[WxiZInlJIV5[2y3c3nvck9ndG:5IHP5eI9u\XS{aXOgZY5idHm|aYOsJGlEPTB;OT64JO69VS5? NUTVTGZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyO|M3OzJpPkK0Nlc{PjN{PD;hQi=>
human NALM6 cells M17PfmN6fG:2b4jpZ:Kh[XO|YYm= M2jSNFczKGh? Ml7LR5l1d3SxeHnjbZR6KGGpYXnud5QhWGhvbnXnZZRqfmViaIXtZY4hVkGOTU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KH[rdHHsJIR6\SCneHPseZNqd25xZnzve{BkgXSxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVkvPiEQvF2u MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ5M{[zNkc,OjR{N{O2N|I9N2F-
human CCRF-CEM cells NF3reVJEgXSxdH;4bYPDqGG|c3H5 NHXNeHE4OiCq NXrpdHFpS3m2b4TvfIlkcXS7IHHnZYlve3RiUHitcoVo[XSrdnWgbJVu[W5iQ1PSSk1ETU1iY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJZqfGGuIHT5[UBmgGOudYPpc44w\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPU[uPEDPxE1w MnXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{N{O2N|IoRjJ2MkezOlMzRC:jPh?=
human SUP-B15 cells MlPJR5l1d3SxeHnjxsBie3OjeR?= MWW3NkBp MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBRcC2yb4PpeIl3\SCqdX3hckBUXVBvQkG1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSC4aYThcEBlgWViZYjjcJV{cW:wL3\sc5ch[3m2b33leJJq[yCjbnHsfZNqeyxiSVO1NF03NjhizszNMi=> NUPuWWhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyO|M3OzJpPkK0Nlc{PjN{PD;hQi=>
human DU145 cells NUjXc4pbS3m2b4TvfIlkyqCjc4PhfS=> NGTjUoY4OiCq NHv4U|hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCjZoTldkA4OiCqcoOgZpkhfmm2YXyg[JlmKGW6Y3z1d4lwdi:obH;3JIN6fG:vZYTybYMh[W6jbInzbZMtKEmFNUC9Ok42KM7:TT6= NHLWPXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK3N|Y{Oid-MkSyO|M3OzJ:L3G+
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mouse bone marrow cells MlLER5l1d3SxeHnjxsBie3OjeR?= Mm\0O|IhcA>? NF25UmlEgXSxdH;4bYNqfHliYXfhbY5{fCCEQ2KtRWJNKG[3c3nvckBxem:2ZXnuJFE6OCCneIDy[ZN{cW6pIH3veZNmKGKxbnWgcYFzem:5IHPlcIx{KGGodHXyJFczKGi{czDifUB3cXSjbDDkfYUh\XilbIXzbY9vN2[ub4egZ5l1d22ndILpZ{BidmGueYPpd{whUUN3ME2zMlMh|ryPLh?= M1jRUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkezOlMzLz5{NEK3N|Y{OjxxYU6=
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mouse MN9D cells MkDXSpVv[3Srb36gZZN{[Xl? NVv4[20xPSEQvF2= MVvJcoR2[3Srb36gc4YhWFB{QTDjZZRidHm2aXOgd5VjfW6rdDDhZ5Rqfmm2eTDpckBud3W|ZTDNUllFKGOnbHzzJIF{e2W|c3XkJIF{KHCqb4PwbIF1\SCuZY\lcEBifCB3IIXN NYPCVFRoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOVAyPjVpPkK1NFUxOTZ3PD;hQi=>
rat PC12 cells Mkf1SpVv[3Srb36gZZN{[Xl? MXy1JO69VQ>? MX6zNEB1dyBzMkCgcYlvew>? NH\3UIZKdmS3Y4Tpc44hd2ZiUGCyRUBk[XSjbIn0bYMhe3WkdX7peEBi[3Srdnn0fUBqdiC{YYSgVGMyOiClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhifGVibHX2[Ywh[XRiNTD1UUBu\WG|dYLl[EA{OCC2bzCxNlAhdWmwcz6= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB3MEG2OUc,OjVyNUCxOlU9N2F-
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BT-12 NECxR2FyUFSVIHHzd4F6 M4\TbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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CHO NWPjWWNGTnWwY4Tpc44h[XO|YYm= NGPtdoZC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHMyWDNicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjZYxkcXWvIH\seZgh[nliYXXxeY9zcW5vZHXybZZm\CCudX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:Oi53MUG4Pe69VS5? NHLlTok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OTR6NUSvK|5EcEWPQly8M4E,
CHO MlzWSpVv[3Srb36gZZN{[Xl? NX;kb4ZGSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBUOVB3IILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZ4Ft[2m3bTDmcJV5KGK7IHHldZVwemmwLXTldol3\WRibIXtbY5me2OnbnPlJIF{e2G7LDDFR|UxRTNwMU[yNljPxE1w NEGx[pk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OTR6NUSvK|5EcEWPQly8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-mTOR / mTOR / p-GSK3β / GSK3β / p-IKKα/β / IKKα / NF-κB / Survivin; 

PubMed: 28717222     


Dose-dependent effects of FTY720 on the phosphorylation of Akt, mTOR, GSK3β, and IKKα/β, and the expression of NF-κB, and survivin in SCC2095 cells. Cells were treated with FTY720 in 5% FBS-supplemented DMEM/F12 medium for 24h, and cell lysates were immunoblotted as described in Material and Methods

p-STAT3 / STAT3 / Bcl-xl / Bcl-2 / Bax ; 

PubMed: 25344679     


CC cells were treated for 24 h with or without FTY720 and analyzed for the indicated protein by western blotting. 

Cyclin D1 / CDK4 / cyclin E / CDK2 / p27 / p16 ; 

PubMed: 25344679     


FTY720 induces expression of p16 and p27 and reduces expression of cyclin D1, CDK4, cyclin E and CDK2. CC cells were treated with FTY720 at the indicated concentrations for 24 h. Lysates were then prepared immediately and analyzed by western blotting for cyclin D1, CDK4, cyclin E, CDK2, p16 and p27. β-Actin was used as the internal control. All assays were done in triplicate. 

28717222 25344679
Immunofluorescence
NF-κB; 

PubMed: 28717222     


Effect of FTY720 on the nuclear translocation of NF-κB. SCC2095 cells were treated with 5μM FTY720 for 24h, stained with anti-NF-κB, and examined by confocal microscopy.

N-cadherin / Vimentin ; 

PubMed: 25344679     


Single and merged images show immunofluorescence staining of N-cadherin (green) and vimentin (red). The cell nucleus is stained blue by DAPI.

28717222 25344679
Growth inhibition assay
Cell viability; 

PubMed: 28717222     


Effect of FTY720 at the indicated concentrations on the viability of oral cancer cells. Cells were treated with FTY720 in 5% FBS-supplemented DMEM/F12 medium in 96- well plates at 24h, and cell viability was assessed by MTT assays. Points, means; bars, S.D. (n=6). *P<0.01 compared to the control group.

28717222
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]

Protocol

Cell Research:[1]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: NOD/SCIDγc−/− mice bearing ALL cells.
  • Dosages: 5 mg/kg/day, 10 mg/kg/day
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL (200.63 mM)
Water 69 mg/mL (200.63 mM)
Ethanol '69 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
20 mg/mL

* 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 Information

Molecular Weight 343.9
Formula

C19H33NO2.HCl

CAS No. 162359-56-0
Storage powder
in solvent
Synonyms N/A
Smiles CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03345940 Terminated 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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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