Fingolimod (FTY720) HCl

Catalog No.S5002

Fingolimod (FTY720) HCl Chemical Structure

Molecular Weight(MW): 343.9

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

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In DMSO USD 91 In stock
USD 97 In stock
USD 170 In stock
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3 Customer Reviews

  •  

     

    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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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 M4TQXGZ2dmO2aX;uJIF{e2G7 MX;B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGOxVFEhemWlZYD0c5Ih\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiY3:t[ZhxemW|c3nu[{BmT0[SIHHzd4V{e2WmIHHzJJJm[2WydH;yJIlvfGW{bnHsbZpifGmxbjDpcpRwKGO7dH;wcIF{dSC3c3nu[{BJd2WlaIP0JIR6\SC|dHHpcolv\yxiRVO1NF0xNjByMjFOwG0v MVOyNlExPDF2NB?=
CHO cells NIq0fHZHfW6ldHnvckBie3OjeR?= NHLYSnNFcXOybHHj[Y1mdnRib3[gX|M{WF2|cHjpcodwe2mwZTCxJJBpd3OyaHH0[UBnem:vIHj1cYFvKFNzUEGgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyxiSVO1NF0xNjh2IN88UU4> M3njXlE2PjF3NUGz
mouse bone marrow cells M3r1XmN6fG:2b4jpZ:Kh[XO|YYm= NHrJR4o4OiCq NGPOOmJEgXSxdH;4bYNqfHliYXfhbY5{fCCEQ2KtRWJNKG[3c3nvckBxem:2ZXnuJFE6OCCneIDy[ZN{cW6pIH3veZNmKGKxbnWgcYFzem:5IHPlcIx{KGGodHXyJFczKGi{czDifUB3cXSjbDDkfYUh\XilbIXzbY9vN2[ub4egZ5l1d22ndILpZ{BidmGueYPpd{whUUN3ME2zMlMh|ryPLh?= M4P5cFI1Ojd|NkOy
human MCF7 cells M33l[3Bzd2yrZnXyZZRqd25iYYPzZZk> M{[5XVc5KGh? M2HhfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3PEBpenNiYomgW3NVNTFiYYPzZZktKEmFNUC9OUDPxE1w NF30b|EzOTR3NkWyOC=>
MDA-MB-231 cells MlrlVJJwdGmoZYLheIlwdiCjc4PhfS=> M1mzU|c5KGh? MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzhiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxRSB3IN88UU4> NUXuO4RtOjF2NU[1NlQ>
human SK-BR-3 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 NIL3SZE4QCCq NVPVSoxnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd6IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1iNTFOwG0v NHjmb4EzOTR3NkWyOC=>
human HCT116 cells NEXDTWlRem:uaX\ldoF1cW:wIHHzd4F6 NH3MOWE4QCCq Mon5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|ghcHK|IHL5JHdUXC1zIHHzd4F6NCCLQ{WwQVUh|ryPLh?= MnzhNlE1PTZ3MkS=
human SW620 cells MnjsVJJwdGmoZYLheIlwdiCjc4PhfS=> M2HuN|c5KGh? NIDiRYhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOlIxKGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFc5KGi{czDifUBYW1RvMTDhd5NigSxiSVO1NF02KM7:TT6= Ml3YNlE1PTZ3MkS=
human BLIN-1 cells NFXUVmFEgXSxdH;4bYPDqGG|c3H5 NGXuSFU4OiCq NHO3ZoxEgXSxdH;4bYNqfHliYXfhbY5{fCCSaD3u[YdifGm4ZTDoeY1idiCETFnOMVEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwNTFOwG0v NIDGdFQzPDJ5M{[zNi=>
human BV173 cells MnPFR5l1d3SxeHnjxsBie3OjeR?= M2HXbVczKGh? NYDSfJB[S3m2b4TvfIlkcXS7IHHnZYlve3RiUHitdI9{cXSrdnWgbJVu[W5iQm[xO|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwMzFOwG0v M{XQfFI1Ojd|NkOy
human DU145 cells NHS2bIxEgXSxdH;4bYPDqGG|c3H5 M{XkPFczKGh? MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC3NkBpenNiYomgeol1[WxiZInlJIV5[2y3c3nvck9ndG:5IHP5eI9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Nj61JO69VS5? NUi3Xnp6OjR{N{O2N|I>
human SUP-B15 cells M1zRW2N6fG:2b4jpZ:Kh[XO|YYm= NHq1WGo4OiCq MnztR5l1d3SxeHnjbZR6KGGpYXnud5QhWGhvcH;zbZRqfmViaIXtZY4hW1WSLVKxOUBk\WyuczDh[pRmeiB5MjDodpMh[nlidnn0ZYwh\HmnIHX4Z4x2e2mxbj;mcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Pi56IN88UU4> MUiyOFI4OzZ|Mh?=
human CCRF-CEM cells NIX1dHVEgXSxdH;4bYPDqGG|c3H5 MYG3NkBp MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBRcC2wZXfheIl3\SCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB5MjDodpMh[nlidnn0ZYwh\HmnIHX4Z4x2e2mxbj;mcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Pi56IN88UU4> NWLac4hDOjR{N{O2N|I>
human NALM6 cells M{W1b2N6fG:2b4jpZ:Kh[XO|YYm= MXy3NkBp MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBRcC2wZXfheIl3\SCqdX3hckBPSUyPNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhfmm2YXyg[JlmKGW6Y3z1d4lwdi:obH;3JIN6fG:vZYTybYMh[W6jbInzbZMtKEmFNUC9PU43KM7:TT6= Mnm3NlQzPzN4M{K=
human PC3 cells Mo\jR5l1d3SxeHnjxsBie3OjeR?= NWD6TXlTPzJiaB?= NH74c29EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJZqfGGuIHT5[UBmgGOudYPpc44w\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUmuPEDPxE1w MnXPNlQzPzN4M{K=
Sf9 insect cells NH7yeVNHfW6ldHnvckBie3OjeR?= NU\GXWxVOSCq NGP1TFJKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGOxVGwhMDZ{IITvJFU3QCliZYjwdoV{e2WmIHnuJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiU{HQJIF{KHO3YoP0doF1\SCjZoTldkAyKGi{ NX\rXopnOjR6MEm4NVQ>
human Jurkat cells NInQb|FHfW6ldHnvckBie3OjeR?= M2fwd|E5KGh? MnnnVoV3\XK|YXygc4YhcW6qaXLpeIlwdiCxZjDtbZRw[2ixbnTybYFtKG[3bnP0bY9vKGmwIHj1cYFvKEq3cnvheEBk\WyuczDh[pRmeiBzODDodpMhcW5icILld4Vv[2Vib3[gXk1XSURvZn3r NEPpTnYyPzRyMEW1OS=>
mouse MN9D cells MVHGeY5kfGmxbjDhd5NigQ>? MnTPNE4yPiEQvF2= M{TLOVczKGh? MX\O[ZVzd3C{b4TlZ5RqfmViYXP0bZZqfHliaX6gcY92e2ViTV65SEBk\WyuczDhd5Nme3OnZDDhd{BjdG:la3nu[{Bw\iCWTl[tZYxxcGFiYYPzc4Nq[XSnZDD0c5hq[2m2eTDheEAxNjF4IIXNJIFnfGW{IEeyJIhzeyCkeTDUdplx[W5iYnz1[UB{fGGrbnnu[{4> MWCyOVA2ODF4NR?=
mouse MN9D cells NHXSPHNHfW6ldHnvckBie3OjeR?= NGPsNpcxNjF4IN88US=> MnXSNlQhcA>? M1vKPG5mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDpckBud3W|ZTDNUllFKGOnbHzzJIF{e2W|c3XkJIF{KHO2aX31cIF1cW:wIH;mJGJFVkZiZYjwdoV{e2mxbjDheEAxNjF4IIXNJIFnfGW{IEK0JIhzew>? MYSyOVA2ODF4NR?=
rat PC12 cells NYDKfFJCTnWwY4Tpc44h[XO|YYm= NX75PGtLPSEQvF2= NYD2d4ZUOzBidH:gNVIxKG2rboO= M4rBOmlv\HWldHnvckBw\iCSUELBJINifGGueYTpZ{B{fWK3bnn0JIFkfGm4aYT5JIlvKHKjdDDQR|EzKGOnbHzzJIF{e2W|c3XkJIF{KHCqb4PwbIF1\SCuZY\lcEBifCB3IIXNJI1m[XO3cnXkJFMxKHSxIEGyNEBucW6|Lh?= NGToXG4zPTB3MEG2OS=>
mouse MN9D cells MmHySpVv[3Srb36gZZN{[Xl? M{\4VVUh|ryP NXLxc3prUW6mdXP0bY9vKG:oIGDQNmEh[2G2YXz5eIlkKHO3YoXubZQh[WO2aY\peJkhcW5ibX;1d4UhVU57RDDj[YxteyCjc4Pld5Nm\CCjczDwbI9{eGijdHWgcIV3\WxiYYSgOUB2VQ>? NVXC[HA2OjVyNUCxOlU>

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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]
+ Expand
  • 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.
    (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 (200.63 mM)
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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01633112 Completed Relapsing-remitting Multiple Sclerosis (RRMS) Novartis Pharmaceuticals|Novartis August 9 2012 Phase 4
NCT01623596 Completed Relapsing Remitting Multiple Sclerosis Novartis Pharmaceuticals|Novartis June 8 2012 Phase 4
NCT00099736 Completed Kidney Transplantation Novartis Pharmaceuticals|Novartis May 7 2003 Phase 3
NCT02373098 Completed Relapsing Remitting Multiple Sclerosis Novartis Pharmaceuticals|Novartis March 31 2015 Phase 4
NCT03345940 Recruiting 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
NCT02342704 Terminated Relapsing-Remitting Multiple Sclerosis Biogen November 30 2014 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID