Fingolimod hydrochloride

Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator

Product information

CAS Number: 162359-56-0

Molecular Weight: 343.93

Formula: C19H34ClNO2

Synonym:

FTY720

FTY-720

FTY 720

Fingolimod

Fingolimod HCl

Gilenia

Gilenya

Related CAS Number:

162359-55-9 (Fingolimod)

Chemical Name: 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1, 3-diol hydrochloride

Smiles: Cl.CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1

InChiKey: SWZTYAVBMYWFGS-UHFFFAOYSA-N

InChi: InChI=1S/C19H33NO2.ClH/c1-2-3-4-5-6-7-8-17-9-11-18(12-10-17)13-14-19(20,15-21)16-22;/h9-12,21-22H,2-8,13-16,20H2,1H3;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 69 mg/mL(200.63 mM). Water: 69 mg/mL(200.63 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.

References:

1. Wallington-Beddoe CT, et al. PLoS One. 2012, 7(5), e36429.
2. Liu Y, et al. Int J Mol Med. 2012, 30(1), 211-219.
3. Rolin J, et al. Cancer Immunol Immunother. 2010, 59(4), 575-586.

Products are for research use only. Not for human use.