Fingolimod (FTY720) HCl

Catalog No.S5002

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 27 Publications

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Ann Neurol, 2014, 76(3):325-37

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PLoS One, 2014, 9(7):e103033

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J Lipid Res, 2013, 54(6):1616-29

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PLoS One, 2013, 8(7): e70124

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J Mol Histol, 2013, 44(6):693-703

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Ren Fail, 2013, 35(7):996-1004

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Transplant Proc, 2013, 45(2):783-6

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Blood, 2012, 119(9):2176-7

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PLoS One, 2012, 7(5):e36429

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PLoS One, 2012, 7(2):e32211

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Mol Med, 2011, 17(7-8):717-25

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Dig Dis Sci, 2011, 56(8):2283-91

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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	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)

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)

References

[4] Nikolova Z, et al. Transpl Immunol. 2001, 8(4), 267-277.

+ Expand

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 Download Fingolimod (FTY720) HCl SDF

Molecular Weight	343.9
Formula	C₁₉H₃₃NO₂.HCl
CAS No.	162359-56-0
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

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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SKI II is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2.
Vismodegib (GDC-0449)

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.
Forskolin

Forskolin is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology.
Cyclopamine

Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
Plerixafor 8HCl (AMD3100 8HCl)

Plerixafor 8HCl (AMD3100 8HCl) is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.
GANT61

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

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Fingolimod (FTY720) HCl

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Fingolimod (FTY720) HCl

Cited by 27 Publications

Purity & Quality Control

Choose Selective S1P Receptor Inhibitors

Biological Activity

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References

Solubility (25°C)

Chemical Information Download Fingolimod (FTY720) HCl SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

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The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

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