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
CAS: 162359-56-0
产品质控
批次：
纯度：
99.99%
99.99
Fingolimod (FTY720) HCl相关产品
| 相关靶点 | S1PR1 S1PR4 S1PR5 S1PR2 | 点击展开 |
|---|---|---|
| 相关产品 | JTE 013 PF 429242 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ GPCR小分子化合物库 | 点击展开 |
相关信号通路图
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 | ||
| 点击查看更多细胞系数据 | |||||
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 |
|
| 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 |
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 (200.63 mM) Ethanol : 69 mg/mL (200.63 mM) |
摩尔浓度计算器 |
|
体内溶解度 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
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
只
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，注：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：取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：取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。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
Tags: buy Fingolimod (FTY720) HCl | Fingolimod (FTY720) HCl supplier | purchase Fingolimod (FTY720) HCl | Fingolimod (FTY720) HCl cost | Fingolimod (FTY720) HCl manufacturer | order Fingolimod (FTY720) HCl | Fingolimod (FTY720) HCl distributor
