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FTY720 (Fingolimod) Hydrochloride S1P Receptor antagonista

Name: FTY720 (Fingolimod) Hydrochloride
Brand: Selleck Chemicals
SKU: S5002
Rating: 5 (136 reviews)

N. Cat.S5002

Fingolimod (FTY720, Fingolimod Hydrochloride) HCl è un antagonista di S1P con IC50 di 0,033 nM nelle cellule K562 e NK. Si prega di usare soluzione salina anziché PBS per le diluzioni. Il PBS può causare precipitazione.

FTY720 (Fingolimod) Hydrochloride S1P Receptor antagonista Chemical Structure

Struttura chimica

Peso molecolare: 343.9

Vai a

Controllo Qualità

Lotto: Purezza: 99.99%

99.99

Target correlati	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Altro S1P Receptor Inibitori	JTE 013 PF 429242 CAY10444 CYM5541 CYM-5520 SEW 2871 SLF1081851 hydrochloride CYM50308 MP-A08 Etrasimod(APD334)

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	PMID
human U2OS cells	Function assay			Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining, EC50=0.002 μM.	22104144
human PC3 cells	Cytotoxic assay		72 h	Cytotoxicity against human PC3 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=9.8 μM.	24273632
human NALM6 cells	Cytotoxic assay		72 h	Cytotoxicity against Ph-negative human NALM6 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=9.6 μM.	24273632
human CCRF-CEM cells	Cytotoxic assay		72 h	Cytotoxicity against Ph-negative human CCRF-CEM cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.8 μM.	24273632
human SUP-B15 cells	Cytotoxic assay		72 h	Cytotoxicity against Ph-positive human SUP-B15 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.8 μM.	24273632
human DU145 cells	Cytotoxic assay		72 h	Cytotoxicity against human DU145 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.5 μM.	24273632
human BV173 cells	Cytotoxic assay		72 h	Cytotoxicity against Ph-positive human BV173 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=6.3 μM.	24273632
human BLIN-1 cells	Cytotoxic assay		72 h	Cytotoxicity against Ph-negative human BLIN-1 cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=5.5 μM.	24273632
mouse bone marrow cells	Cytotoxic assay		72 h	Cytotoxicity against BCR-ABL fusion protein 190 expressing mouse bone marrow cells after 72 hrs by vital dye exclusion/flow cytometric analysis, IC50=3.3 μM.	24273632
Sf9 insect cells	Function assay		1 h	Inhibition of human recombinant S1PL (62 to 568) expressed in Sf9 insect cells using S1P as substrate after 1 hr	24809814
mouse MN9D cells	Function assay	5 μM		Induction of PP2A catalytic subunit activity in mouse MN9D cells assessed as phosphate level at 5 uM	25050165
rat PC12 cells	Function assay	5 μM	30 to 120 mins	Induction of PP2A catalytic subunit activity in rat PC12 cells assessed as phosphate level at 5 uM measured 30 to 120 mins.	25050165
mouse MN9D cells	Function assay	0.16 μM	24 h	Neuroprotective activity in mouse MN9D cells assessed as stimulation of BDNF expression at 0.16 uM after 24 hrs	25050165
mouse MN9D cells	Function assay	0.16 μM	72 h	Neuroprotective activity in mouse MN9D cells assessed as blocking of TNF-alpha associated toxicity at 0.16 uM after 72 hrs by Trypan blue staining.	25050165
CHO	Function assay			Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells, IC50=0.84μM.	15615513
CHO	Function assay			Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells, IC50=2.1μM.	15615513
Jurkat	Function assay		18 hrs	Reversal of inhibition of mitochondrial function in human Jurkat cells after 18 hrs in presence of Z-VAD-fmk	17400555
T-cells	Function assay		96 hrs	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, IC50=0.0061μM.	21456524
SK-BR-3	Antiproliferative assay		78 hrs	Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5μM.	21456524
MDA-MB-231	Antiproliferative assay		78 hrs	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5μM.	21456524
HCT116	Antiproliferative assay		78 hrs	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5μM.	21456524
SW620	Antiproliferative assay		78 hrs	Antiproliferative activity against human SW620 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5μM.	21456524
MCF7	Antiproliferative assay		78 hrs	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5μM.	21456524
LNCAP-AI	Antiproliferative assay		78 hrs	Antiproliferative activity human LNCAP-AI cells assessed as growth inhibition after 78 hrs by WST-1 assay, IC50=5μM.	21456524
MGC803	Antitumor assay	10 mg/kg	20 days	Antitumor activity against human MGC803 cells xenografted in nude mouse assessed as inhibition of tumor growth at 10 mg/kg for 20 days	21456524
U2OS	Function assay		18 hrs	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, EC50=0.0072μM.	26687487
FL5.12A	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse FL5.12A cells after 48 hrs by DAPI staining-based flow cytometric analysis, IC50=2.4μM.	27475534
SH-SY5Y	Cytotoxicity assay		24 hrs	Cytotoxicity against human SH-SY5Y cells measured after 24 hrs by crystal-violet staining based assay, EC10=0.54μM.	27913115
SK-N-SH	Cytotoxicity assay		24 hrs	Cytotoxicity against human SK-N-SH cells measured after 24 hrs by crystal-violet staining based assay, EC10=0.55μM.	27913115
U118MG	Cytotoxicity assay		24 hrs	Cytotoxicity against human U118MG cells measured after 24 hrs by crystal-violet staining based assay, EC10=0.61μM.	27913115
SH-SY5Y	Function assay			Agonist activity at sphingosine-1-phosphate receptor in human SH-SY5Y cells assessed as increase in cAMP level at EC10 by direct immunoassay	27913115
U118MG	Function assay			Agonist activity at sphingosine-1-phosphate receptor in human U118MG cells assessed as increase in cAMP level at EC10 by direct immunoassay	27913115
SK-N-SH	Function assay			Agonist activity at sphingosine-1-phosphate receptor human SK-N-SH cells assessed as increase in cAMP level at EC10 by direct immunoassay	27913115
HEK293	Function assay		18 hrs	Agonist activity at sphingosine-1-phosphate receptor (unknown origin) expressed in HEK293 cells assessed as increase in cAMP level at EC10 after 18 hrs by CRE-responsive renilla luciferase reporter gene assay	27913115
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
FL5.12	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse FL5.12 cells after 48 hrs by DAPI or propidium iodide staining-based flow cytometric analysis, IC50=2.1μM.	30292898
FL5.12	Cytotoxicity assay	10 uM	3 hrs	Cytotoxicity against mouse FL5.12 cells assessed as vacuole formation at 10 uM after 3 hrs by fluorescence microscopic analysis	30292898
FL5.12	Cytotoxicity assay	2.5 uM	3 hrs	Cytotoxicity against mouse FL5.12 cells assessed as vacuole formation at 2.5 uM after 3 hrs by fluorescence microscopic analysis	30292898
HepG2	qHTS assay			HepG2 cells viability qHTS for Zika virus inhibitors	33229545
CHO	Function assay			Agonist activity at human S1P3 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay, EC50=2.51189μM.	ChEMBL
CHO	Function assay			Agonist activity at human S1P5 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay, EC50=3.16228μM.	ChEMBL
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	343.9	Formula	C₁₉H₃₃NO₂.HCl	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	162359-56-0	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	Fingolimod Hydrochloride,FTY720			Smiles	CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl

Solubilità

In vitro
Lotto:

DMSO : 69 mg/mL (200.63 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	3.450mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL 69 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	S1P receptor (K562, NK cells ) 0.033 nM
In vitro	L'effetto inibitorio di S1P è rovesciato da varie concentrazioni di FTY720, con un effetto IC50 di 173 nM. Inoltre, FTY720 (10 nM) da solo non esercita alcun effetto sull'espressione delle molecole co-stimolatorie. FTY720 inverte l'aumento dell'espressione di HLA-I indotto da S1P sia per le percentuali di cellule che per il MFI, confrontando l'effetto di S1P con l'effetto della combinazione di S1P con FTY720. FTY720-P a dosi medie e alte migliora anche i livelli di TGF-β1. L'espressione di mRNA di TGF-β1 e Foxp3 è sovraregolata nel gruppo FTY720-P a dose alta. La proliferazione delle cellule T effettrici è soppressa significativamente nel gruppo FTY720-P a dosi medie e alte con un rapporto cellule Treg/Teff di 1:1. Con un rapporto di 1:1, la proliferazione delle cellule T effettrici è soppressa anche nel gruppo FTY720 a dose alta.
In vivo	FTY720 è efficace nei xenotrapianti di ALL Ph⁺ ma non Ph^- utilizzando un modello di malattia precoce. FTY720 produce una significativa riduzione del carico di malattia nei xenotrapianti di ALL Ph⁺ utilizzando un modello di malattia precoce. I xenotrapianti di ALL Ph⁺ umani rispondono a FTY720 con una riduzione dell'80% della malattia complessiva se il trattamento è stato iniziato precocemente. Al contrario, il trattamento di topi con FTY720 non comporta una riduzione della leucemia rispetto ai controlli utilizzando quattro xenotrapianti di ALL Ph^- umani separati.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/19823820/ [2] https://pubmed.ncbi.nlm.nih.gov/22576630/ [3] https://pubmed.ncbi.nlm.nih.gov/22570713/ [4] https://pubmed.ncbi.nlm.nih.gov/11316070/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	p-AKT / AKT / p-mTOR / mTOR / p-GSK3β / GSK3β / p-IKKα/β / IKKα / NF-κB / Survivin p-STAT3 / STAT3 / Bcl-xl / Bcl-2 / Bax Cyclin D1 / CDK4 / cyclin E / CDK2 / p27 / p16	28717222
Immunofluorescence	NF-κB N-cadherin / Vimentin	28717222
Growth inhibition assay	Cell viability	28717222

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT05141669	Completed	Multiple Sclerosis	Novartis Pharmaceuticals\|Novartis	May 18 2020	--
NCT03345940	Terminated	Relapsing Remitting Multiple Sclerosis	Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta\|Patient-Centered Outcomes Research Institute\|Universita degli Studi di Genova	April 30 2017	Phase 4
NCT02575365	Terminated	Cognition\|Brain Volume Loss	Novartis Pharmaceuticals\|Novartis	February 16 2016	Phase 4

Supporto tecnico

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