Cat. No.: HY-11063

Fingolimod

(Synonyms: FTY720 free base)

78 Cited Publications

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Based on 78 publication(s) in Google Scholar

Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC₅₀ of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.97%
CAS No.: 162359-55-9
Formule: C₁₉H₃₃NO₂
Masse moléculaire:307.47

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fingolimod Chemical Structure

CAS No.: 162359-55-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (78)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
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Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

S1P

0.033 nM (IC₅₀, in K562 and NK cells)

PAK1

Voir tous les produits spécifiques à Isoform LPL Receptor :

Voir tous les produits spécifiques à Isoform PAK :

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	IC₅₀	3.3 μM Compound: 1, FTY720	Cytotoxicity against BCR-ABL fusion protein 190 expressing mouse bone marrow cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against BCR-ABL fusion protein 190 expressing mouse bone marrow cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
BT-474	IC₅₀	8.5 μM Compound: 37; FTY720	Cytotoxicity against human BT-474 cells assessed as inhibition of cell growth incubated for 24 hrs by MTS assay Cytotoxicity against human BT-474 cells assessed as inhibition of cell growth incubated for 24 hrs by MTS assay	[PMID: 37974956]
BV-173	IC₅₀	6.3 μM Compound: 1, FTY720	Cytotoxicity against Ph-positive human BV173 cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against Ph-positive human BV173 cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
CCRF-CEM	IC₅₀	6.8 μM Compound: 1, FTY720	Cytotoxicity against Ph-negative human CCRF-CEM cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against Ph-negative human CCRF-CEM cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
CHO	IC₅₀	>10000 nM Compound: 1, FTY-720	Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	>10000 nM Compound: 1, FTY-720	Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	2100 nM Compound: 1, FTY-720	Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	840 nM Compound: 1, FTY-720	Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	>10000 nM Compound: 1, FTY-720	Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells	[PMID: 15615513]
CHO	EC₅₀	>10000 nM Compound: 1	Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	>10000 nM Compound: 1	Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	>10000 nM Compound: 1	Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	>10000 nM Compound: 1	Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	>10000 nM Compound: 1	Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
DU-145	IC₅₀	6.5 μM Compound: 1, FTY720	Cytotoxicity against human DU145 cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against human DU145 cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
FL5.12	IC₅₀	2.4 μM Compound: 1; FTY720	Cytotoxicity against mouse FL5.12A cells after 48 hrs by DAPI staining-based flow cytometric analysis Cytotoxicity against mouse FL5.12A cells after 48 hrs by DAPI staining-based flow cytometric analysis	[PMID: 27475534]
FL5.12	IC₅₀	2.1 μM Compound: 1	Cytotoxicity against mouse FL5.12 cells after 48 hrs by DAPI or propidium iodide staining-based flow cytometric analysis Cytotoxicity against mouse FL5.12 cells after 48 hrs by DAPI or propidium iodide staining-based flow cytometric analysis	[PMID: 30292898]
HCT-116	IC₅₀	5 μM Compound: 1, FTY-720, Gilenya	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 78 hrs by WST-1 assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 78 hrs by WST-1 assay	[PMID: 21456524]
MCF7	IC₅₀	5 μM Compound: 1, FTY-720, Gilenya	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 78 hrs by WST-1 assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 78 hrs by WST-1 assay	[PMID: 21456524]
MDA-MB-231	IC₅₀	5 μM Compound: 1, FTY-720, Gilenya	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 78 hrs by WST-1 assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 78 hrs by WST-1 assay	[PMID: 21456524]
MDA-MB-231	IC₅₀	2.9 μM Compound: 37; FTY720	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 24 hrs by MTS assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 24 hrs by MTS assay	[PMID: 37974956]
NALM-6	IC₅₀	9.6 μM Compound: 1, FTY720	Cytotoxicity against Ph-negative human NALM6 cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against Ph-negative human NALM6 cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
PC-3	IC₅₀	9.8 μM Compound: 1, FTY720	Cytotoxicity against human PC3 cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against human PC3 cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
Sf9	IC₅₀	17 μM Compound: 1, FTY720	Inhibition of human recombinant S1PL (62 to 568) expressed in Sf9 insect cells using S1P as substrate after 1 hr Inhibition of human recombinant S1PL (62 to 568) expressed in Sf9 insect cells using S1P as substrate after 1 hr	[PMID: 24809814]
SH-SY5Y	IC₅₀	4.71 μM Compound: Fingolimod	Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]
SK-BR-3	IC₅₀	5 μM Compound: 1, FTY-720, Gilenya	Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition after 78 hrs by WST-1 assay Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition after 78 hrs by WST-1 assay	[PMID: 21456524]
SK-N-AS	IC₅₀	6.11 μM Compound: Fingolimod	Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]
SUP-B15	IC₅₀	6.8 μM Compound: 1, FTY720	Cytotoxicity against Ph-positive human SUP-B15 cells after 72 hrs by vital dye exclusion/flow cytometric analysis Cytotoxicity against Ph-positive human SUP-B15 cells after 72 hrs by vital dye exclusion/flow cytometric analysis	[PMID: 24273632]
SW-620	IC₅₀	5 μM Compound: 1, FTY-720, Gilenya	Antiproliferative activity against human SW620 cells assessed as growth inhibition after 78 hrs by WST-1 assay Antiproliferative activity against human SW620 cells assessed as growth inhibition after 78 hrs by WST-1 assay	[PMID: 21456524]
T-cell	IC₅₀	6.1 nM Compound: 1, FTY-720, Gilenya	Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay	[PMID: 21456524]
U2OS	EC₅₀	0.002 μM Compound: 2b, FTY720	Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining	[PMID: 22104144]
U2OS	EC₅₀	7.2 nM Compound: FTY720; Gilenya	Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay	[PMID: 26687487]
U2OS	EC₅₀	>10000 nM Compound: FTY720; Gilenya	Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay	[PMID: 26687487]

In Vitro

The monocyte-derived immature dendritic cells (iDCs) are pretreated with various concentrations of S1P for various periods of time prior to their incubation with NK cells. Four hours incubation of autologous or allogeneic iDCs with 0.2-20 μM of S1P significantly protectes these cells from NK cell lysis. The IC₅₀ values of S1P are calculated at 160 nM for autologous iDCs, and 34 nM for allogeneic iDCs. Next, the inhibitory effect of S1P is revered by various concentrations of Fingolimod or SEW2871, with an IC₅₀ effect of 173 or 15 nM, respectively^[1]. Fingolimod has been reported to reduce LPA synthesis via inhibition of the lysophospholipase autotaxin. Fingolimod treatment correlates with a significant elevation of axonal cAMP, a crucial factor for axonal outgrowth. Additionally, Fingolimod significantly reduces LPA levels in the injured nerve. PF-8380 treatment correlates with improved myelin thickness^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Fingolimod treatment results in significantly increased nerve conduction at 14 days post-crush in wildtype C57BL/6 mice. However, Foxn1^-/- mice, which are devoid of T- but not B-lymphocytes, show an improvement of nerve regeneration under fingolimod treatment. Although the mean increase in nerve conduction velocity in both fingolimod-treated and controlFoxn1^-/- mice implies a potentially positive role of T-lymphocyte deficiency on nerve regeneration, only fingolimod-treated Foxn1^-/- mice show a significant improvement compared to C57BL/6 controls and performed better in the functional analysis^[2]. Treatment of the animals with Fingolimod for 28 d results in a clear reduction in the binding of ¹⁸F-GE180 when compare with vehicle-treated animals and evaluated by ex vivo autoradiography. Quantification of the binding of the radiotracer revealed a significant reduction in the binding potential of ¹⁸F-GE180 (P<0.0001) after treatment with Fingolimod^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 162359-55-9
Appearance Solid
Masse moléculaire 307.47
Formule C₁₉H₃₃NO₂
Color White to off-white
SMILES

OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)CO
Synonyms

FTY720 free base
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (78)

All Cell Proliferation/Viability AssayHistological Imaging/StainingFlow CytometryIn Vivo Efficacy StudyWBIHC

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Journal Impact Factor

Signal Transduct Target Ther

Intranasal prime-boost RNA vaccination elicits potent T cell response for lung cancer therapy. [Abstract]

2025 Mar 24;10(1):101. PMID: 40122855
Nature

Dietary cysteine enhances intestinal stemness via CD8+ T cell-derived IL-22. [Abstract]

2025 Nov;647(8090):706-715. PMID: 41034585
Cancer Cell

Targeting P4HA1 promotes CD8+ T cell progenitor expansion toward immune memory and systemic anti-tumor immunity. [Abstract]

2025 Feb 10;43(2):213-231.e9. PMID: 39729997
Cell Metab

Quercetin-derived microbial metabolite DOPAC potentiates CD8+ T cell anti-tumor immunity via NRF2-mediated mitophagy. [Abstract]

2025 Oct 24:S1550-4131(25)00395-X. PMID: 41138722
Nat Genet

TGF-β builds a dual immune barrier in colorectal cancer by impairing T cell recruitment and instructing immunosuppressive SPP1+ macrophages. [Abstract]

2025 Dec;57(12):3050-3065. PMID: 41203813
Immunity

Small-molecule CBP/p300 histone acetyltransferase inhibition mobilizes leukocytes from the bone marrow via the endocrine stress response. [Abstract]

2024 Feb 13;57(2):364-378.e9. PMID: 38301651

Fingolimod purchased from MedChemExpress. Usage Cited in: Immunity. 2024 Feb 13;57(2):364-378.e9. [Abstract]

Dynamic changes in blood leukocytes and neutrophils upon Firategrast (0.2 mg/kg; i.p.) or vehicle treatment expressed as percentage of the mean cell count at baseline.
Cell Res

Comprehensive metabolomics expands precision medicine for triple-negative breast cancer. [Abstract]

2022 May;32(5):477-490. PMID: 35105939
Cancer Res

Metronomic Chemotherapy Induces Metabolic Reprogramming in Cancer Cells That Modulates Mature Regulatory Dendritic Cell Function to Stimulate Antitumor Immunity. [Abstract]

2026 Mar 5. PMID: 41784618
Nat Commun

TCF-1 and TOX regulate the memory formation of intestinal group 2 innate lymphoid cells in asthma. [Abstract]

2024 Sep 8;15(1):7850. PMID: 39245681
Nat Commun

Glycolysis inhibition induces anti-tumor central memory CD8+T cell differentiation upon combination with microwave ablation therapy. [Abstract]

2024 May 31;15(1):4665. PMID: 38821965
Nat Commun

SLAM-family receptors promote resolution of ILC2-mediated inflammation. [Abstract]

2024 Jun 13;15(1):5056. PMID: 38871792
Nat Commun

Overcoming resistance to immune checkpoint therapy in PTEN-null prostate cancer by intermittent anti-PI3Kα/β/δ treatment. [Abstract]

2022 Jan 10;13(1):182. PMID: 35013322
Autophagy

Metabolic stress induces a double-positive feedback loop between AMPK and SQSTM1/p62 conferring dual activation of AMPK and NFE2L2/NRF2 to synergize antioxidant defense. [Abstract]

2024 Nov;20(11):2490-2510. PMID: 38953310
Adv Sci (Weinh)

Dnmt1 Alleviates S1PR1-Mediated Pyroptosis after Spinal Cord Injury through Regulating Pon3 Expression. [Abstract]

2025 Aug 30:e07330. PMID: 40884250
Adv Sci (Weinh)

PP2Ac Regulates Autophagy via Mediating mTORC1 and ULK1 During Osteoclastogenesis in the Subchondral Bone of Osteoarthritis. [Abstract]

2024 Jul 23:e2404080. PMID: 39041921
Cardiovasc Res

Periaortic lymphatic vessels protect against thoracic aortic dissection through mobilizing immune response. [Abstract]

2025 Nov 11:cvaf215. PMID: 41213294
Theranostics

Tertiary lymphoid organs are associated with the progression of kidney damage and regulated by interleukin-17A. [Abstract]

2021 Jan 1;11(1):117-131. PMID: 33391465
Hum Reprod Open

Hypoxia exposure impairs male fertility via inhibiting Septin2-mediated spermatogonial proliferation. [Abstract]

2025 May 14;2025(3):hoaf027. PMID: 40487848

Fingolimod purchased from MedChemExpress. Usage Cited in: Hum Reprod Open. 2025 May 14;2025(3):hoaf027. [Abstract]

Treatment with Fingolimod (FTY720) (2 mg/kg;i.p.; once daily for 35 days) exacerbated the negative impact of hypoxia on fertility in male mice, as evidenced by worsened seminiferous epithelium.

Fingolimod purchased from MedChemExpress. Usage Cited in: Hum Reprod Open. 2025 May 14;2025(3):hoaf027. [Abstract]

Fingolimod (FTY720) (2 mg/kg;i.p.; once daily for 35 days) significantly reduced sperm count and motility and increased sperm deformity rate in hypoxic mice.
Nat Cardiovasc Res

The TRPM7 chanzyme in smooth muscle cells drives abdominal aortic aneurysm in mice. [Abstract]

2025 Feb;4(2):216-234. PMID: 39953275
Research (Wash D C)

Early Growth Response Gene 1 Benefits Autoimmune Disease by Promoting Regulatory T Cell Differentiation as a Regulator of Foxp3. [Abstract]

2025 Apr 15:8:0662. PMID: 40235598

Fingolimod purchased from MedChemExpress. Usage Cited in: Research (Wash D C). 2025 Apr 15:8:0662. [Abstract]

Fingolimod (FTY-720) (1 mg/kg) apparently elevated the ratio of CD4⁺Egr-1⁺ cells in lymph nodes of EAE mice.

Fingolimod purchased from MedChemExpress. Usage Cited in: Research (Wash D C). 2025 Apr 15:8:0662. [Abstract]

H&E and LFB staining showed inflammatory infiltration in the spinal cord. Fingolimod (FTY-720) (1 mg/kg) alleviated spinal cord inflammatory infiltration and demyelination in ERE-EGFP mice with EAE.
J Immunother Cancer

Liver-directed AAV-IL-10 therapy enhances CD8+ T cell-mediated immunity against hepatocellular carcinoma. [Abstract]

2026 Mar 27;14(3):e012460. PMID: 41895716
J Immunother Cancer

Anti-galectin-9 therapy synergizes with EGFR inhibition to reprogram the tumor microenvironment and overcome immune evasion. [Abstract]

2025 Jul 15;13(7):e010926. PMID: 40664443
J Immunother Cancer

Reinforcing cancer immunotherapy with engineered porous hollow mycobacterium tuberculosis loaded with tumor neoantigens. [Abstract]

2025 Feb 6;13(2):e010150. PMID: 39915006
Cell Rep Med

Glycoengineering-based anti-PD-1-iRGD peptide conjugate boosts antitumor efficacy through T cell engagement. [Abstract]

2024 Jun 18;5(6):101590. PMID: 38843844
Cancer Lett

Targeting Galectin-9 to overcome immunosuppression and potentiate ATR inhibitor therapy. [Abstract]

2026 Apr 10:643:218283. PMID: 41651398
Cancer Lett

FTY720 enhances the anti-tumor activity of carboplatin and tamoxifen in a patient-derived xenograft model of ovarian cancer. [Abstract]

2018 Nov 1:436:75-86. PMID: 30120964

Fingolimod purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Nov 1:436:75-86. [Abstract]

Immunoblotsof sphingolipid metabolizing enzymes SPHK1, SPHK2, acid ceramidase (AC), and glucosylceramide synthase (GCS) in A2780. cp20, SKOV3. TR, HeyA8. MDR, COV362, and CAOV3 cell lines exposed to the indicated concentrations of FTY720 (FTY) or DMSO (VC) for 24 h.

Fingolimod purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Nov 1:436:75-86. [Abstract]

FTY720+ICI 47699 and FTY720+NSC 241240 increase apoptosis marker, cleaved caspase 3 in a PDX model of EOC. IHC of tumor sections is used to detect the apoptosis marker cleaved caspase 3 and the cell cycle inhibitor p21.
Cell Death Dis

S1PR3-driven positive feedback loop sustains STAT3 activation and keratinocyte hyperproliferation in psoriasis. [Abstract]

2025 Jan 20;16(1):31. PMID: 39833165
Phytomedicine

Alisol A 24-acetate protects against NASH-associated fibrosis via suppression of Kupffer cell-derived SPHK1/S1P axis. [Abstract]

2025 Sep 19:148:157271. PMID: 40992063
Phytomedicine

Ginsenoside F2-modified liposomes delivering FTY720 enhance glioblastoma targeting and antitumor activity via ferroptosis. [Abstract]

2025 May 30:144:156917. PMID: 40480023
Phytomedicine

Unveiling XinJia-LuHuang Granules' protective mechanism against atherosclerosis: Integrating network pharmacology, metabolomics, and experimental validation. [Abstract]

2025 May 27:143:156919. PMID: 40466509
Haematologica

Human BCR/ABL1 induces chronic myeloid leukemia-like disease in zebrafish. [Abstract]

2020 Mar;105(3):674-686. PMID: 31289206
J Med Chem

Systems Biology-Based Drug Repositioning Identifies Extracellular Matrix Module as a Therapeutic Target in Lung Squamous Cell Carcinoma. [Abstract]

2025 Oct 17. PMID: 41105954
J Med Chem

A Novel Compound 3a-M1, from Metabolites of Sinomenine Derivative 3a, Exerts Potent Anti-Aplastic Anemia Activity via IP3R/ORAI-Mediated CTL Ferroptosis. [Abstract]

2025 Apr 17. PMID: 40243551
Breast Cancer Res

Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade. [Abstract]

2017 Aug 4;19(1):90. PMID: 28778177

Fingolimod purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2017 Aug 4;19(1):90. [Abstract]

The effect of ZD1839-FTY720 treatment on CD44 expression in TNBC cell lines. HCC1806, Hs578T, and MDA-MB-468 TNBC cell lines at ~40% confluence in 12-well plates are exposed for 24 h to ZD1839 (Gef: 0.1 to 10 μM), with or without the addition of 1.5 μM FTY720.
Cancer Immunol Immunother

Tumor-draining lymph nodes respond to immune checkpoint inhibition and orchestrate tumor immune remodeling. [Abstract]

2025 Oct 6;74(11):326. PMID: 41051631
Cancer Immunol Immunother

Microwave ablation combined with immune checkpoint inhibitor enhanced the antitumor immune activation and memory in rechallenged tumor mouse model. [Abstract]

2025 Mar 25;74(5):161. PMID: 40131498
Commun Biol

A genome-scale CRISPR Cas9 dropout screen identifies synthetically lethal targets in SRC-3 inhibited cancer cells. [Abstract]

2021 Mar 25;4(1):399. PMID: 33767353
Life Sci

FTY720 inhibits the activation of pancreatic stellate cells by promoting apoptosis and suppressing autophagy via the AMPK/mTOR pathway. [Abstract]

2019 Jan 15:217:243-250. PMID: 30550889
Biomolecules

Notch Signaling Exacerbates Pulmonary Fibrosis by Regulating the Differentiation of CD4+ Tissue-Resident Memory T Cells. [Abstract]

2026 Feb 20;16(2):328. PMID: 41750395
Front Pharmacol

Pien Tze Huang Alleviates Relapsing-Remitting Experimental Autoimmune Encephalomyelitis Mice by Regulating Th1 and Th17 Cells. [Abstract]

2018 Oct 31:9:1237. PMID: 30429789
Int Immunopharmacol

FTY720 alleviates HBV-mediated inflammatory liver injury through a dual role of inhibiting lymphocyte trafficking and viral replication. [Abstract]

2025 Mar 22:153:114495. PMID: 40121743
Int Immunopharmacol

CD83 mediates the inhibitory effect of the S1PR1 agonist CYM5442 on LPS-induced M1 polarization of macrophages through the ERK-STAT-1 signaling pathway. [Abstract]

2024 Oct 31;143(Pt 3):113526. PMID: 39486189
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845
Am J Physiol Cell Physiol

Glycolytic enzyme PFKFB3 regulates sphingosinae 1-phosphate receptor 1 in proangiogenic glomerular endothelial cells under diabetic condition. [Abstract]

2023 Nov 1;325(5):C1354-C1368. PMID: 37781737
Eur J Pharmacol

Geniposide inhibits SphK1 membrane targeting to restore macrophage polarization balance in collagen-induced arthritis mice. [Abstract]

2022 Oct 15:933:175271. PMID: 36108735
J Mol Cell Cardiol

Ventricular SK2 upregulation following angiotensin II challenge: Modulation by p21-activated kinase-1. [Abstract]

2022 Mar:164:110-125. PMID: 34774547
Int Immunopharmacol

Prophylactic administration of fingolimod (FTY720) ameliorated experimental autoimmune myasthenia gravis by reducing the number of dendritic cells, follicular T helper cells and antibody-secreting cells. [Abstract]

2021 Jul:96:107511. PMID: 33915521
RSC Adv

Carboxymethylcellulose encapsulated fingolimod, siRNA@ZnO hybrid nanocomposite as a new anti-Alzheimer's material. [Abstract]

2024 Jul 12;14(30):22044-22055. PMID: 39006767
Front Endocrinol

Nuclear Insulin-Like Growth Factor Binding Protein-3 As a Biomarker in Triple-Negative Breast Cancer Xenograft Tumors: Effect of Targeted Therapy and Comparison With Chemotherapy. [Abstract]

2018 Mar 22:9:120. PMID: 29623068
Mol Neurobiol

Teriflunomide Promotes Blood-Brain Barrier Integrity by Upregulating Claudin-1 via the Wnt/β-catenin Signaling Pathway in Multiple Sclerosis. [Abstract]

2024 Apr;61(4):1936-1952. PMID: 37819429
Helicobacter

Vaccine-induced gastric CD4+ tissue-resident memory T cells proliferate in situ to amplify immune response against Helicobacter pylori insult. [Abstract]

2019 Oct;24(5):e12652. PMID: 31414552
BMC Microbiol

Fingolimod as a potent anti-Staphylococcus aureus: pH-dependent cell envelope damage and eradication of biofilms/persisters. [Abstract]

2025 May 16;25(1):299. PMID: 40380090
FASEB J

SPHK1/S1P/S1PR pathway promotes the progression of peritoneal fibrosis by mesothelial-mesenchymal transition. [Abstract]

2024 Jan 31;38(2):e23417. PMID: 38226856
J Inflamm Res

Fingolimod Suppresses NLRP3 Inflammasome Activation and Alleviates Oxidative Stress in Traumatic Brain Injury-Induced Acute Lung Injury. [Abstract]

2025 Feb 14:18:2229-2245. PMID: 39974815
J Pharmacol Exp Ther

Targeting cholangiocyte sphingosine-1-phosphate (S1P) receptor 1 signaling alleviates cholestatic liver injury: Mechanistic insight into S1P/phosphorylated signal transducer and activator of transcription 3 axis. [Abstract]

2026 Apr;393(4):104306. PMID: 41818851
Cell Signal

Hedgehog pathway inhibitor HhAntag suppresses virus infection via the GLI-S1PR axis. [Abstract]

2025 Apr 15:132:111807. PMID: 40239727
Mol Hum Reprod

Stage-dependent sphingosine-1-phosphate pathway modulation as a therapeutic strategy in a murine model of adenomyosis. [Abstract]

2026 Feb 16:gaag009. PMID: 41698850
Reprod Biomed Online

Blocking sphingosine 1-phosphate receptor 1 with modulators reduces immune cells infiltration and alleviates endometriosis in mice. [Abstract]

2023 Nov;47(5):103304. PMID: 37757611
J Immunol

Hepatitis B Virus Increases SphK1-S1P Synthesis by Promoting the Availability of the Transcription Factor USF1. [Abstract]

2024 Nov 15;213(10):1499-1507. PMID: 39400236
Wound Repair Regen

Drug suspending during wound healing effectively weakens immunosuppression-related complications by preserving CD8+ T cell function. [Abstract]

2023 Jul-Aug;31(4):489-499. PMID: 37129099
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
J Gastroenterol Hepatol

Amelioration of colitis through blocking lymphocytes entry to Peyer's patches by sphingosine-1-phosphate lyase inhibitor. [Abstract]

2018 Jan 15. PMID: 29336057
Clin Rheumatol

PP2A dysfunction mediated by PPP2R1A deficiency drives cGAS-STING-dependent hyperinflammation in SLE CD14+ monocytes. [Abstract]

2026 Mar;45(3):1709-1720. PMID: 41582267
J Integr Neurosci

Fingolimod Alleviates Inflammation after Cerebral Ischemia via HMGB1/TLR4/NF-κB Signaling Pathway. [Abstract]

2024 Aug 12;23(8):142. PMID: 39207074
Vet Microbiol

Lipid metabolism is a novel and practical source of potential targets for antiviral discovery against porcine parvovirus. [Abstract]

2021 Oct:261:109177. PMID: 34391196
Curr Eye Res

FTY720 Suppresses Pathogenic Retinal Müller Cell Activation and Chronic Progression by Inhibiting the mTOR/NF-κB Signaling Pathway and Regulating Autophagy. [Abstract]

2024 Aug;49(8):862-871. PMID: 38577836
BMC Res Notes

A genome-wide CRISPR/Cas9 screen reveals novel positive regulators of FTY720 sensitivity in acute lymphoblastic leukemia cells. [Abstract]

2026 Jan 23;19(1):75. PMID: 41578398
Biomed Chromatogr

Liquid chromatography-tandem mass spectrometry for determination of fingolimod and its active metabolite fingolimod phosphate in whole blood of patients with multiple sclerosis. [Abstract]

2024 Jun 26:e5947. PMID: 38932506
Res Sq

2026 Jun 2.
bioRxiv

2026 Apr 30.
bioRxiv

Therapeutic scheduling of WEE1 inhibition preserves T cell function and promotes immune control of HPV+ tumors. [Abstract]

2026 Mar 17:2026.03.10.710574. PMID: 41889874
bioRxiv

Indomethacin exerts both cyclooxygenase inhibition-dependent and independent mechanisms to enhance chemo-immunotherapy in mice. [Abstract]

2026 Jan 8:2026.01.07.698231. PMID: 41542639
Res Sq

2024 Oct 18.
Research Square Preprint

2024 Apr 23.
Research Square Preprint

2023 Dec 1.
Research Square Preprint

2023 Sep 6.
J Immunol Sci

March 31, 2022.
Patent

US20210393524A1.

Solvant et solubilité

In Vitro:

Ethanol : 7.69 mg/mL (25.01 mM; Need ultrasonic)

DMSO : 2 mg/mL (6.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2523 mL

16.2617 mL

32.5235 mL

5 mM

0.6505 mL

3.2523 mL

6.5047 mL

10 mM

0.3252 mL

1.6262 mL

3.2523 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil

Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Immature dendritic cells (DCs) are left intact or are incubated with 2 μM S1P, 10 nM Fingolimod, 10 nM SEW2871 or the combinations of S1P with these drugs for 4 h. 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]^[3]

Mice^[2]
Rag1^-/- mice(B6.129S7-Rag1^tm1Mom/J), Foxn1^-/- mice (B6.Cg/NTac-Foxn1^nu) mice, and control C57BL/6 mice are used. Mice receive non-phosphorylated Fingolimod via intraperitoneal injection at a concentration of 1 mg/kg once daily over the course of 16 days, starting 2 days before crush until 14 days post-crush. PF-8380 is dissolved in DMSO and administered at a concentration of 10 mg/kg via intraperitoneal injection once daily, as well starting 2 days before until 14 days post-crush. Controls receive an equal volume of solvent.
Rats^[3]
Male Lewis rats (50-100 g, n=18) are used. After the peripheral activation of the lesion, the DTH EAE lesions are allowed to develop until day 127 to generate large chronic lesions and the animals are then treated for 28 d with either Fingolimod (n=7) or vehicle (n=7). The Fingolimod treatment is given daily (0.3 mg/kg in 0.5 mL of water). The control group is given water (0.5 mL) as a vehicle control. The animals are dosed via oral gavage to ensure accurate dosing. In this model, the acute inflammation subsides after day 20 of activation of the lesion, and the BBB damage subsides. Thus, at day 127 the lesion clearly represents a well-developed chronic MS lesion. PET imaging is performed immediately before initiation of treatment and at the end of the treatment period.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Rolin J, et al. FTY720 and SEW2871 reverse the inhibitory effect of S1P on natural killer cell mediated lysis of K562 tumor cells and dendritic cells but not on cytokine release. Cancer Immunol Immunother. 2010, 59(4), 575-586. [Content Brief]

[2]. Szepanowski F, et al. Fingolimod promotes peripheral nerve regeneration via modulation of lysophospholipid signaling. J Neuroinflammation. 2016 Jun 10;13(1):143. [Content Brief]

[3]. Airas L, et al. In vivo PET imaging demonstrates diminished microglial activation after fingolimod treatment in an animal model of multiple sclerosis. J Nucl Med. 2015 Feb;56(2):305-10. [Content Brief]

[4]. Shirakabe K, et al. Modification of lymphocyte migration to Peyer's patches by inhibition of sphingosine-1-phosphate lyase ameliorates murine colitis. J Gastroenterol Hepatol. 2018 Jan 15. [Content Brief]

[5]. Hunter S F, et al. The direct effects of fingolimod in the central nervous system: implications for relapsing multiple sclerosis[J]. CNS drugs, 2016, 30(2): 135-147.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	3.2523 mL	16.2617 mL	32.5235 mL	81.3087 mL
DMSO / Ethanol	5 mM	0.6505 mL	3.2523 mL	6.5047 mL	16.2617 mL
Ethanol	10 mM	0.3252 mL	1.6262 mL	3.2523 mL	8.1309 mL
	15 mM	0.2168 mL	1.0841 mL	2.1682 mL	5.4206 mL
	20 mM	0.1626 mL	0.8131 mL	1.6262 mL	4.0654 mL
	25 mM	0.1301 mL	0.6505 mL	1.3009 mL	3.2523 mL

Keywords

Fingolimod

78 Cited Publications

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Chemical Information

Publications (78)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fingolimod Related Classifications

HY-11063 Related Classifications