Free shipping on all orders over $ 500

FTY720

Cat. No. M1712
FTY720 Structure
Synonym:

Fingolimod

Size Price Availability Quantity
100mg USD 75 In stock
200mg USD 125 In stock
1g USD 280 In stock
5g USD 750 In stock
Bulk Inquiry?

Quality Control
Biological Activity

FTY720 (Fingolimod) is a sphingosine-1-phosphate receptor 1 receptor. FTY720 is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). FTY720 (Fingolimod) also mediated antitumor effects in hepatocellular carcinoma (HCC) cells by activating PKC. The three HCC cell lines examined, Hep3B, Huh7, and PLC5, exhibited differential susceptibility to FTY720-mediated suppression of cell viability, with IC50 values of 4.5, 6.3, and 11 μM, respectively.

Protocol
Cell Experiment
Cell lines MCF-7 cells
Preparation method In Vitro Proliferation Assay Cells were seeded onto 96- well plates at the densities of 3000 cells/well. After 24 h of pre-cultivation, appropriate concentrations of the samples were added and the cells were cultured for 2 d. The relative growth ratio was determined by WST-1 assay using a cell counting kit (Dojindo Laboratories, Kumamoto, Japan) according to the manufacturer’s instructions. The IC50 value was determined from the dose response curve. At least three independent experiments were performed. The proliferation assay that tested the effects of DMS was performed using identical methods. Compounds with or without DMS were added to the wells and the plates were incubated for 78 h at 37 °C in a humidified atmosphere containing 5% CO2 before the WST-1 assay was conducted.
Concentrations 0~100µM
Incubation time 2 days
Animal Experiment
Animal models Six-weekold female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice with Mino cells
Formulation not mentioned
Dosages 10 mg/kg daily for 10 days
Administration intraperitoneal injections
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 343.9
Formula C19H33NO2.HCl
CAS Number 162359-56-0
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Neuropharmacology (2017). Figure 6. FTY720 (AbMole BioScience, Kowloon, Hong Kong, China)
Method Immunoblots
Cell Lines OLN-93 cells
Concentrations 160 nM
Incubation Time 12 h
Results On immunoblots we noted that 12 h of 160 nM FTY720 treatment of OLN-93 cells produced a significant increase in global acetylation of histone 3 (AcH3)
Rating
Source Neuropharmacology (2017). Figure 4. FTY720 (AbMole BioScience, Kowloon, Hong Kong, China)
Method qPCR
Cell Lines OLN-93 cells
Concentrations 160 nM
Incubation Time 12 h
Results Empty vector transfected cells expressed BDNF (Fig. 4A, lane 1) and 12 h treatments with 160 nM FTY720 significantly increased BDNF expression in all stably transfected aSyn OLN-93 cell lines (Fig. 4A, lanes 3, 5 and 7), visualized on agarose gels showing the BDNF amplicons generated by qPCR.
Rating
Source Neuropharmacology (2017). Figure 2. FTY720 (AbMole BioScience, Kowloon, Hong Kong, China)
Method qPCR
Cell Lines OLN-93 cells
Concentrations 160 nM
Incubation Time 12 h
Results Similar to our earlier assessment in neuronal cells (Vargas-Medrano et al., 2014), we found that using 160 nM FTY720 treatment of OLN-93 cells for 12 h significantly increased BDNF expression as measured using qPCR (Fig. 2, dark gray whisker box).
Rating
Product Citations
References

Fingolimod (FTY720) inhibits neuroinflammation and attenuates spontaneous convulsions in lithium-pilocarpine induced status epilepticus in rat model.
Gao et al. Pharmacol Biochem Behav. 2012 Aug 31. PMID: 22960129.

Fingolimod in the treatment algorithm of relapsing remitting multiple sclerosis: a statement of the Central and East European (CEE) MS Expert Group.
Fazekas F. Wien Med Wochenschr. 2012 Aug;162(15-16):354-366. PMID: 22895849.

Fingolimod, a sphingosine-1 phosphate receptor modulator, increases BDNF levels and improves symptoms of a mouse model of Rett syndrome.
Deogracias et al. Proc Natl Acad Sci U S A. 2012 Aug 28;109(35):14230-5. PMID: 22891354.

Development of oral agent in the treatment of multiple sclerosis: how the first available oral therapy, fingolimod will change therapeutic paradigm approach.
Gasperini et al. Drug Des Devel Ther. 2012;6:175-86. PMID: 22888218.

Related Src-bcr-Abl Products
Radotinib

Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.

Dasatinib Monohydrate

Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

Dasatinib HCl

Dasatinib(BMS-354825) hydrochloride is a potent and dual Abl/ Src inhibitor IC50 of <1 nM/0.8 nM respectively; also inhibit c-Kit (WT)/c-Kit (D816V) with IC50 of 79 nM/37 nM.

MCB-613

MCB-613 is a potent steroid receptor coactivator (SRC) stimulator.

GNF-7

GNF-7 is the first type II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design next generation Bcr-Abl kinase inhibitors.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: FTY720, Fingolimod supplier, Src-bcr-Abl, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.