Fingolimod (FTY-720)

Catalog No.S5950 Batch:S595003

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Technical Data

Formula

C19H33NO2
Molecular Weight 307.47 CAS No. 162359-55-9
Solubility (25°C)* In vitro DMSO 61 mg/mL (198.39 mM)
Ethanol 31 mg/mL (100.82 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
1.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
Targets
S1P receptor [1]
In vitro

The main immunomodulatory mechanism of action of fingolimod is based on its effect on lymphocyte homing. It reversibly redistributes T and B cells from the circulation to secondary lymphoid organs like peripheral and mesenteric lymph nodes and Peyer's patches, thereby causing a state of peripheral lymphopenia[1].
In vivo

SphK2 is the only enzyme which activates fingolimod in vivo,since only Sphk2 knockout mice are resistant to fingolimod-induced lymphopenia. A major advantage of fingolimod as a therapeutic agent is the possibility of its oral application. Absorption is food-independent and slow (maximal plasma concentration after 12-16 h), but extensive, and its bioavailability is high (93%). It reaches steady state concentrations after 1-2 months during daily intake. Fingolimod shows high plasma protein binding (>99.7%), mainly to albumin, and in contrast to S1P, there is no evidence for fingolimod binding to ApoM/HDL. It has a large volume of distribution of approx. 20L/kg and shows slow blood clearance (6.3±2.3 L/h), resulting in a half-life of 6-9 days[1].

Fingolimod alleviates disease burden in immune-mediated animal models of multiple sclerosis[2].

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    NSCLC cells

  • Concentrations

    10 μM

  • Incubation Time

    72 h

  • Method

    Cells were treated with various concentrations of drug for 72 h.
Animal Study:

[2]
  • Animal Models

    C57/B6 mice

  • Dosages

    1 mg/kg

  • Administration

    o.g.

Selleck's Fingolimod (FTY-720) has been cited by 23 publications

A novel isoxazole compound CM2-II-173 inhibits the invasive phenotype of triple-negative breast cancer cells [ Oncol Res, 2023, 31(6):867-875] PubMed: 37744269
Selective delivery of low-affinity IL-2 to PD-1+ T cells rejuvenates antitumor immunity with reduced toxicity [ J Clin Invest, 2022, 132(3)e153604] PubMed: 35104810
Selective delivery of low-affinity IL-2 to PD-1+ T cells rejuvenates antitumor immunity with reduced toxicity [ J Clin Invest, 2022, 132(3)e153604] PubMed: 35104810
Intratumoral administration of STING-activating nanovaccine enhances T cell immunotherapy [ J Immunother Cancer, 2022, 10(5)e003960] PubMed: 35623658
The central role of Sphingosine kinase 1 in the development of neuroendocrine prostate cancer (NEPC): A new targeted therapy of NEPC [ Clin Transl Med, 2022, 12(2):e695] PubMed: 35184376
The sphingosine kinase inhibitor SKI-V suppresses cervical cancer cell growth [ Int J Biol Sci, 2022, 18(7):2994-3005] PubMed: 35541904
Targeting sphingosine kinase 1/2 by a novel dual inhibitor SKI-349 suppresses non-small cell lung cancer cell growth [ Cell Death Dis, 2022, 13(7):602] PubMed: 35831279
Efficacy of Vafidemstat in Experimental Autoimmune Encephalomyelitis Highlights the KDM1A/RCOR1/HDAC Epigenetic Axis in Multiple Sclerosis [ Pharmaceutics, 2022, 14(7)1420] PubMed: 35890315
The immunostimulatory RNA RN7SL1 enables CAR-T cells to enhance autonomous and endogenous immune function [ Cell, 2021, 184(19):4981-4995.e14] PubMed: 34464586
ChenThe interplay between fibroblast-like synovial and vascular endothelial cells leads to angiogenesis via the sphingosine-1-phosphate-induced RhoA-F-Actin and Ras-Erk1/2 pathways and the intervention of geniposide [ Phytother Res, 2021, 10.1002/ptr.7211] PubMed: 34327764

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.