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

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FTY720 (Fingolimod) Hydrochloride S1P Receptor 길항제

제품 번호S5002

Fingolimod (FTY720, Fingolimod Hydrochloride) HCl은 K562 및 NK 세포에서 IC50 0.033 nM을 갖는 S1P 길항제입니다. 희석에는 PBS 대신 생리 식염수를 사용하십시오. PBS는 침전을 일으킬 수 있습니다.
FTY720 (Fingolimod) Hydrochloride S1P Receptor 길항제 Chemical Structure

화학 구조

분자량: 343.9

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품질 관리

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도

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

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

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

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

S1P의 억제 효과는 다양한 농도의 FTY720에 의해 역전되며, IC50 효과는 173 nM입니다. 또한 FTY720 (10 nM) 단독으로는 공동 자극 분자 발현에 영향을 미치지 않습니다. FTY720은 S1P 단독 효과와 S1P와 FTY720을 함께 사용한 효과를 비교했을 때, 세포 비율과 MFI 모두에서 S1P에 의해 유도된 HLA-I 발현 증가를 역전시킵니다. 중간 및 고용량 FTY720-P는 또한 TGF-β1 수치를 증가시킵니다. 고용량 FTY720-P 그룹에서는 TGF-β1 및 Foxp3 mRNA 발현이 상향 조절됩니다. Treg/Teff 세포 비율이 1:1일 때, 중간 및 고용량 FTY720-P 그룹에서 이펙터 T 세포의 증식이 유의하게 억제됩니다. 1:1 비율에서 고용량 FTY720 그룹에서도 이펙터 T 세포의 증식이 억제됩니다.

생체 내(In vivo)

FTY720은 초기 질병 모델을 사용하는 Ph+ 급성 림프구성 백혈병(ALL) 이종이식편에서는 효과적이지만 Ph- ALL 이종이식편에서는 효과적이지 않습니다. FTY720은 초기 질병 모델을 사용하는 Ph+ ALL 이종이식편에서 질병 부담을 유의하게 감소시킵니다. Ph+ 인간 ALL 이종이식편은 치료가 조기에 시작되었을 경우 FTY720에 반응하여 전체 질병이 80% 감소합니다. 대조적으로, FTY720으로 마우스를 치료해도 4개의 별개의 인간 Ph- ALL 이종이식편을 사용한 대조군에 비해 백혈병이 감소하지 않습니다.

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

적용 분야

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

(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

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