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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Cited by 27 Publications

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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 MkK3SpVv[3Srb36gZZN{[Xl? MYnB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGOxVFEhemWlZYD0c5Ih\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiY3:t[ZhxemW|c3nu[{BmT0[SIHHzd4V{e2WmIHHzJJJm[2WydH;yJIlvfGW{bnHsbZpifGmxbjDpcpRwKGO7dH;wcIF{dSC3c3nu[{BJd2WlaIP0JIR6\SC|dHHpcolv\yxiRVO1NF0xNjByMjFOwG0v MWeyNlExPDF2NB?=
CHO cells MlvTSpVv[3Srb36gZZN{[Xl? M4LUPGRqe3CuYXPlcYVvfCCxZjDbN|NRZXOyaHnu[49{cW6nIEGgdIhwe3CqYYTlJIZzd21iaIXtZY4hWzGSMTDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{NCCLQ{WwQVAvQDRizszNMi=> NHL6PFYyPTZzNUWxNy=>
mouse bone marrow cells M3zwNGN6fG:2b4jpZ:Kh[XO|YYm= MVi3NkBp M{\vNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKFUj3BRmwh\nW|aX;uJJBzd3SnaX6gNVkxKGW6cILld5NqdmdibX;1d4Uh[m:wZTDtZZJzd3diY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJZqfGGuIHT5[UBmgGOudYPpc44w\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUOuN{DPxE1w Mo\qNlQzPzN4M{K=
human MCF7 cells MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 Mn:0O|ghcA>? NFTKNplCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|ghcHK|IHL5JHdUXC1zIHHzd4F6NCCLQ{WwQVUh|ryPLh?= NEfIO2szOTR3NkWyOC=>
MDA-MB-231 cells NE\HXGtRem:uaX\ldoF1cW:wIHHzd4F6 MmXNO|ghcA>? M4TKcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5ODDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTB;IEWg{txONg>? NYTwRmdoOjF2NU[1NlQ>
human SK-BR-3 cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 MoPLO|ghcA>? M{DMcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utRnIuOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4QCCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:KDVizszNMi=> NH63VXYzOTR3NkWyOC=>
human HCT116 cells NX;iN3VxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYW3PEBp Mki0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|ghcHK|IHL5JHdUXC1zIHHzd4F6NCCLQ{WwQVUh|ryPLh?= MnzZNlE1PTZ3MkS=
human SW620 cells MlKwVJJwdGmoZYLheIlwdiCjc4PhfS=> MVi3PEBp MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEe4JIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3ME21JO69VS5? NWL1XpM1OjF2NU[1NlQ>
human BLIN-1 cells M1rObGN6fG:2b4jpZ:Kh[XO|YYm= NFzZeI84OiCq M37vVmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCqLX7l[4F1cX[nIHj1cYFvKEKOSV6tNUBk\WyuczDh[pRmeiB5MjDodpMh[nlidnn0ZYwh\HmnIHX4Z4x2e2mxbj;mcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:PS53IN88UU4> M1znclI1Ojd|NkOy
human BV173 cells NIjoO3REgXSxdH;4bYPDqGG|c3H5 NFS1VlE4OiCq M3\Ob2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCqLYDvd4l1cX[nIHj1cYFvKEKYMUezJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC4aYThcEBlgWViZYjjcJV{cW:wL3\sc5ch[3m2b33leJJq[yCjbnHsfZNqeyxiSVO1NF03NjNizszNMi=> Moq5NlQzPzN4M{K=
human DU145 cells NFrFT5BEgXSxdH;4bYPDqGG|c3H5 M4S1OFczKGh? NFH6SndEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCjZoTldkA4OiCqcoOgZpkhfmm2YXyg[JlmKGW6Y3z1d4lwdi:obH;3JIN6fG:vZYTybYMh[W6jbInzbZMtKEmFNUC9Ok42KM7:TT6= NH[2PHozPDJ5M{[zNi=>
human SUP-B15 cells M4LReGN6fG:2b4jpZ:Kh[XO|YYm= Mk\VO|IhcA>? MoDrR5l1d3SxeHnjbZR6KGGpYXnud5QhWGhvcH;zbZRqfmViaIXtZY4hW1WSLVKxOUBk\WyuczDh[pRmeiB5MjDodpMh[nlidnn0ZYwh\HmnIHX4Z4x2e2mxbj;mcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Pi56IN88UU4> MVOyOFI4OzZ|Mh?=
human CCRF-CEM cells NES4SJFEgXSxdH;4bYPDqGG|c3H5 NUnXd3l3PzJiaB?= Mn[0R5l1d3SxeHnjbZR6KGGpYXnud5QhWGhvbnXnZZRqfmViaIXtZY4hS0OURj3DSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwODFOwG0v M1O2OFI1Ojd|NkOy
human NALM6 cells NYjKZ5k3S3m2b4TvfIlkyqCjc4PhfS=> NH3KWVQ4OiCq MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBRcC2wZXfheIl3\SCqdX3hckBPSUyPNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhfmm2YXyg[JlmKGW6Y3z1d4lwdi:obH;3JIN6fG:vZYTybYMh[W6jbInzbZMtKEmFNUC9PU43KM7:TT6= Mly4NlQzPzN4M{K=
human PC3 cells MVLDfZRwfG:6aXRCpIF{e2G7 M2rDTFczKGh? MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTlwODFOwG0v M3f4b|I1Ojd|NkOy
Sf9 insect cells NIjOWpBHfW6ldHnvckBie3OjeR?= NGnBTYwyKGh? NEPadHFKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGOxVGwhMDZ{IITvJFU3QCliZYjwdoV{e2WmIHnuJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiU{HQJIF{KHO3YoP0doF1\SCjZoTldkAyKGi{ Mmm2NlQ5ODl6MUS=
human Jurkat cells MVXGeY5kfGmxbjDhd5NigQ>? MVSxPEBp M17PfXJmfmW{c3HsJI9nKGmwaHnibZRqd25ib3[gcYl1d2Oqb37kdolidCCodX7jeIlwdiCrbjDoeY1idiCMdYLrZZQh[2WubIOgZYZ1\XJiMUigbJJ{KGmwIIDy[ZNmdmOnIH;mJHouXkGGLX\tby=> M3vyUVE4PDByNUW1
mouse MN9D cells M{\kXGZ2dmO2aX;uJIF{e2G7 NFvnOm8xNjF4IN88US=> MX[3NkBp M3u3WG5mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDpckBud3W|ZTDNUllFKGOnbHzzJIF{e2W|c3XkJIF{KGKub3PrbY5oKG:oIGTOSk1idHCqYTDhd5Nw[2mjdHXkJJRwgGmlaYT5JIF1KDBwMU[geW0h[W[2ZYKgO|IhcHK|IHL5JHRzgXCjbjDicJVmKHO2YXnubY5oNg>? MkXHNlUxPTBzNkW=
mouse MN9D cells MXPGeY5kfGmxbjDhd5NigQ>? M3rTT|AvOTZizszN NIewO2kzPCCq NWLSdYNuVmW3cn;wdo91\WO2aY\lJIFkfGm4aYT5JIlvKG2xdYPlJG1PQURiY3XscJMh[XO|ZYPz[YQh[XNic4TpcZVt[XSrb36gc4YhSkSQRjDlfJBz\XO|aX;uJIF1KDBwMU[geW0h[W[2ZYKgNlQhcHK| MoS2NlUxPTBzNkW=
rat PC12 cells M37UZmZ2dmO2aX;uJIF{e2G7 MnO3OUDPxE1? NEDXepI{OCC2bzCxNlAhdWmwcx?= NIfURopKdmS3Y4Tpc44hd2ZiUGCyRUBk[XSjbIn0bYMhe3WkdX7peEBi[3Srdnn0fUBqdiC{YYSgVGMyOiClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhifGVibHX2[Ywh[XRiNTD1UUBu\WG|dYLl[EA{OCC2bzCxNlAhdWmwcz6= MoSzNlUxPTBzNkW=
mouse MN9D cells NYLBeFJKTnWwY4Tpc44h[XO|YYm= Mk\yOUDPxE1? MmDYTY5lfWO2aX;uJI9nKFCSMlGgZ4F1[Wy7dHnjJJN2[nWwaYSgZYN1cX[rdImgbY4hdW:3c3WgUW46TCClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhifGVibHX2[Ywh[XRiNTD1US=> MYeyOVA2ODF4NR?=

... 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
NCT03257358 Recruiting Relapsing Multiple Sclerosis Novartis Pharmaceuticals|Novartis September 19 2017 Phase 4
NCT03257358 Recruiting Relapsing Multiple Sclerosis Novartis Pharmaceuticals|Novartis September 19 2017 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
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
NCT02956200 Unknown status Stroke|Inflammation Second Affiliated Hospital School of Medicine Zhejiang University November 2016 Phase 2
NCT02956200 Unknown status Stroke|Inflammation Second Affiliated Hospital School of Medicine Zhejiang University November 2016 Phase 2

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S1P Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID