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FTY720 (Fingolimod) Hydrochloride S1P Receptor antagonista

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

Cat. No.S5002

Fingolimod (FTY720, Fingolimod Hydrochloride) HCl es un antagonista de S1P con una IC50 de 0,033 nM en células K562 y NK. Por favor, utilice solución salina en lugar de PBS para las diluciones. El PBS puede causar precipitación.

FTY720 (Fingolimod) Hydrochloride S1P Receptor antagonista Chemical Structure

Estructura química

Peso molecular: 343.9

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Control de calidad

Lote: Pureza: 99.99%

99.99

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

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	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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Información química, almacenamiento y estabilidad

Peso molecular	343.9	Fórmula	C₁₉H₃₃NO₂.HCl	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	162359-56-0	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Fingolimod Hydrochloride,FTY720			Smiles	CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl

Solubilidad

In vitro
Lote:

DMSO : 69 mg/mL (200.63 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC₅₀/Ki	S1P receptor (K562, NK cells ) 0.033 nM
In vitro	El efecto inhibidor del S1P es revertido por diversas concentraciones de FTY720, con un efecto IC50 de 173 nM. Además, el FTY720 (10 nM) por sí solo no ejerce ningún efecto sobre la expresión de moléculas coestimuladoras. El FTY720 revierte el aumento de la expresión de HLA-I inducido por S1P tanto para los porcentajes de células como para el MFI, al comparar el efecto del S1P con el efecto de la combinación de S1P con FTY720. Las dosis medias y altas de FTY720-P también aumentan los niveles de TGF-β1. La expresión de ARNm de TGF-β1 y Foxp3 se regula al alza en el grupo de FTY720-P de dosis alta. La proliferación de las células T efectoras se suprime significativamente en el grupo de FTY720-P de dosis media y alta con una relación de células Treg/Teff de 1:1. Con una relación de 1:1, la proliferación de las células T efectoras también se suprime en el grupo de FTY720 de dosis alta.
In vivo	El FTY720 es eficaz en los xenoinjertos de LLA Ph⁺ pero no en los Ph^- utilizando un modelo de enfermedad temprana. El FTY720 produce una reducción significativa de la carga de la enfermedad en los xenoinjertos de LLA Ph⁺ utilizando un modelo de enfermedad temprana. Los xenoinjertos humanos de LLA Ph⁺ responden al FTY720 con una reducción del 80 % de la enfermedad general si el tratamiento se ha iniciado de forma temprana. En contraste, el tratamiento de ratones con FTY720 no da como resultado una reducción de la leucemia en comparación con los controles utilizando cuatro xenoinjertos humanos de LLA Ph^- separados.
Referencias	[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/

Aplicaciones

Métodos	Biomarcadores	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

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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

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