Home GPCR & G Protein S1P Receptor antagonist FTY720 (Fingolimod) Hydrochloride

연구용

FTY720 (Fingolimod) Hydrochloride S1P Receptor antagonist

제품 번호: S5002

Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.
FTY720 (Fingolimod) Hydrochloride S1P Receptor antagonist Chemical Structure

화학 구조

분자량: 343.9

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품질 관리 (Quality Control)

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 343.9 화학식

C19H33NO2.HCl

 보관 (수령일로부터)
CAS 번호 162359-56-0 SDF 다운로드 원액 보관

동의어 Fingolimod Hydrochloride,FTY720 Smiles CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 69 mg/mL (200.63 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
S1P receptor
(K562, NK cells )
0.033 nM
시험관 내(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.

생체 내(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.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/11316070/

적용 분야 (Applications)

방법 바이오마커 이미지 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
S5002-WB1
28717222
Immunofluorescence NF-κB N-cadherin / Vimentin
S5002-IF1
28717222
Growth inhibition assay Cell viability
S5002-viability1
28717222

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
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