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FTY720 hydrochloride

Cat. No. M1712
FTY720 hydrochloride Structure
Synonym:

Fingolimod

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
100mg USD 53  USD53 In stock
200mg USD 80  USD80 In stock
500mg USD 140  USD140 In stock
1g USD 180  USD180 In stock
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Quality Control
Biological Activity

Fingolimod (FTY720) HCl is a 1-phospho-neuraminol S1P receptor antagonist with an IC50 of 0.33 nM. , FTY720 can dephosphorylate AMPK by activating PP2A and reduce the expression level of phosphorylated eEF2K, ultimately leading to ADCD and iron death in human multiple myeloma cells.

Product Citations
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)
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.
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).
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 343.9
Formula C19H33NO2.HCl
CAS Number 162359-56-0
Purity 99.46%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] Cipriani R, et al. J Neuroinflammation. FTY720 attenuates excitotoxicity and neuroinflammation.

[2] Gao et al. Pharmacol Biochem Behav. Fingolimod (FTY720) inhibits neuroinflammation and attenuates spontaneous convulsions in lithium-pilocarpine induced status epilepticus in rat model.

[3] Fazekas F. Wien Med Wochenschr. Fingolimod in the treatment algorithm of relapsing remitting multiple sclerosis: a statement of the Central and East European (CEE) MS Expert Group.

[4] Deogracias et al. Proc Natl Acad Sci U S A. Fingolimod, a sphingosine-1 phosphate receptor modulator, increases BDNF levels and improves symptoms of a mouse model of Rett syndrome.

[5] Gasperini et al. Drug Des Devel Ther. Development of oral agent in the treatment of multiple sclerosis: how the first available oral therapy, fingolimod will change therapeutic paradigm approach.

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

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