Fingolimod (FTY720) HCl

别名: Fingolimod Hydrochloride,FTY720 中文名称:盐酸芬戈莫德

稀释此产品请用生理盐水,请勿用PBS稀释,可能产生沉淀。

Fingolimod (FTY720, Fingolimod Hydrochloride) HCl是一种S1P拮抗剂,在K562 和 NK细胞中IC50为0.33 nM。 稀释请用生理盐水,请勿用PBS稀释,可能产生沉淀。

Fingolimod (FTY720) HCl Chemical Structure

Fingolimod (FTY720) HCl Chemical Structure

CAS: 162359-56-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 747.57 现货
100mg RMB 806.22 现货
1g RMB 2620.99 现货
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客户使用Selleck的Fingolimod (FTY720) HCl发表文献122

产品质控

批次: 纯度: 99.99%
99.95

Fingolimod (FTY720) HCl相关产品

相关信号通路图

S1P Receptor抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
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
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
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
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
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
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 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
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
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 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 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 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 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 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
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
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
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
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
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
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
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
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
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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生物活性

产品描述 Fingolimod (FTY720, Fingolimod Hydrochloride) HCl是一种S1P拮抗剂,在K562 和 NK细胞中IC50为0.33 nM。 稀释请用生理盐水,请勿用PBS稀释,可能产生沉淀。
靶点
S1P receptor [1]
(K562, NK cells )
0.033 nM
体外研究(In Vitro)
体外研究活性

S1P 作用于K562细胞,抑制NK细胞裂解。多种浓度 FTY720可逆转S1P的抑制作用,IC50为173 nM。此外, 10 nM FTY720 单独温育时,对共刺激分子的表达没有任何影响。通过比较S1P的作用效果与S1P和 FTY720联合作用效果,FTY720 可逆转S1P诱导的 HLA-I 表达提高,同时对于细胞百分数和MFI。[1]培养基和高剂量 FTY720-P也增强 TGF-β1水平。在高剂量FTY720-P 组别中可上调TGF-β1 和 Foxp3 mRNA的表达。在培养基和高剂量FTY720-P 组别中的效应 T(Teff)细胞增殖受抑制,Treg/Teff细胞比率为1:1。比率为1:1时,高剂量 FTY720 组别中的Teff细胞也受抑制。[2]

细胞实验 细胞系 未成熟的 DCs
浓度 10 nM
孵育时间 4 小时
方法

未成熟的 DCs原封不动,或与 2 μM S1P, 10 nM FTY720, 10 nM SEW2871或S1P 与这些药剂的联和温育4小时。使用1 μg/mL LPS作为对照。冲洗细胞,在96孔板(v-型底,每孔 2 × 105 个细胞)中温育,再次冲洗,再悬浮在含0.1%叠氮化钠的 PBS buffer 中。使用1 μg/mL FITC标记的小鼠抗人CD80, CD83, CD86, HLA-class I, HLA-DR, 1 μg/mL HLA-E标记, 使用1 μg/mL FITC标记的小鼠 IgG 作为对照。细胞冲洗两次,在流式细胞仪中检测。根据同型对照 FITC标记的小鼠IgG进行标记。使用多种NK 细胞激活受体的抗体对NK细胞进行染色,或使细胞原封不动或与 2 μM S1P 温育4小时,冲洗,使用1 μg/mL PE标记的小鼠抗人NKp30 (CD337), NKp44 (CD336), NKG2D (CD314),在4 oC下染色45分钟,使用1 μg/mL PE标记的小鼠IgG1作为对照。也使用1 μg/mL FITC标记的抗-杀伤抑制性受体(KIR)/CD158 抗体(识别KIR2DL2, KIR2DL3, KIR2DS2 和KIR2DS4)对NK细胞进行染色,使用FITC标记的小鼠 IgG作为对照。冲洗细胞两次,在流式细胞仪中检测。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot Cyclin D1 / CDK4 / cyclin E / CDK2 / p27 / p16 p-STAT3 / STAT3 / Bcl-xl / Bcl-2 / Bax p-AKT / AKT / p-mTOR / mTOR / p-GSK3β / GSK3β / p-IKKα/β / IKKα / NF-κB / Survivin 25344679
Immunofluorescence N-cadherin / Vimentin NF-κB 25344679
Growth inhibition assay Cell viability 28717222
体内研究(In Vivo)
体内研究活性

FTY720 治疗使用早期疾病模型Ph+而不是 Ph- ALL移植瘤,效果是肯定的。 FTY720 作用于使用早期疾病模型的Ph+ ALL移植瘤,显著降低疾病负担。在所有早期疾病中,FTY720处理的Ph+人类ALL移植瘤降低80±12%。相反, FTY720处理小鼠,与对照组相比,使用四组分开独立的人类 Ph- ALL 移植瘤,减少白血病发生率。[3]

动物实验 Animal Models 携带ALL细胞的NOD/SCIDγc−/−小鼠
Dosages 5 mg/kg/day, 10 mg/kg/day
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

化学信息&溶解度

分子量 343.9 分子式

C19H33NO2.HCl

CAS号 162359-56-0 SDF Download Fingolimod (FTY720) HCl SDF
Smiles CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 69 mg/mL ( 200.63 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : 69 mg/mL

Ethanol : 69 mg/mL

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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