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Fingolimod (FTY720) HCl
別名: Fingolimod Hydrochloride,FTY720 中文名稱：鹽酸芬戈莫德
稀釋此產(chǎn)品請用生理鹽水，請勿用PBS稀釋，可能產(chǎn)生沉淀。
Fingolimod (FTY720, Fingolimod Hydrochloride) HCl是一種S1P拮抗劑，在K562 和 NK細胞中IC50為0.33 nM。 稀釋請用生理鹽水，請勿用PBS稀釋，可能產(chǎn)生沉淀。
Fingolimod (FTY720) HCl Chemical Structure
CAS: 162359-56-0
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Fingolimod (FTY720) HCl相關(guān)產(chǎn)品
| 相關(guān)靶點 | S1PR1 S1PR4 S1PR5 S1PR2 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | JTE 013 PF 429242 | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I GPCR小分子化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Fingolimod (FTY720, Fingolimod Hydrochloride) HCl是一種S1P拮抗劑，在K562 和 NK細胞中IC50為0.33 nM。 稀釋請用生理鹽水，請勿用PBS稀釋，可能產(chǎn)生沉淀。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | S1P 作用于K562細胞，抑制NK細胞裂解。多種濃度 FTY720可逆轉(zhuǎn)S1P的抑制作用，IC50為173 nM。此外, 10 nM FTY720 單獨溫育時，對共刺激分子的表達沒有任何影響。通過比較S1P的作用效果與S1P和 FTY720聯(lián)合作用效果，F(xiàn)TY720 可逆轉(zhuǎn)S1P誘導的 HLA-I 表達提高，同時對于細胞百分數(shù)和MFI。[1]培養(yǎng)基和高劑量 FTY720-P也增強 TGF-β1水平。在高劑量FTY720-P 組別中可上調(diào)TGF-β1 和 Foxp3 mRNA的表達。在培養(yǎng)基和高劑量FTY720-P 組別中的效應 T(Teff)細胞增殖受抑制，Treg/Teff細胞比率為1:1。比率為1:1時,高劑量 FTY720 組別中的Teff細胞也受抑制。[2] |
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|---|---|---|---|---|
| 細胞實驗 | 細胞系 | 未成熟的 DCs | ||
| 濃度 | 10 nM | |||
| 孵育時間 | 4 小時 | |||
| 方法 | 未成熟的 DCs原封不動，或與 2 μM S1P, 10 nM FTY720, 10 nM SEW2871或S1P 與這些藥劑的聯(lián)和溫育4小時。使用1 μg/mL LPS作為對照。沖洗細胞，在96孔板(v-型底,每孔 2 × 105 個細胞)中溫育,再次沖洗，再懸浮在含0.1%疊氮化鈉的 PBS buffer 中。使用1 μg/mL FITC標記的小鼠抗人CD80, CD83, CD86, HLA-class I, HLA-DR, 1 μg/mL HLA-E標記, 使用1 μg/mL FITC標記的小鼠 IgG 作為對照。細胞沖洗兩次，在流式細胞儀中檢測。根據(jù)同型對照 FITC標記的小鼠IgG進行標記。使用多種NK 細胞激活受體的抗體對NK細胞進行染色，或使細胞原封不動或與 2 μM S1P 溫育4小時，沖洗，使用1 μg/mL PE標記的小鼠抗人NKp30 (CD337), NKp44 (CD336), NKG2D (CD314),在4 oC下染色45分鐘，使用1 μg/mL PE標記的小鼠IgG1作為對照。也使用1 μg/mL FITC標記的抗-殺傷抑制性受體(KIR)/CD158 抗體（識別KIR2DL2, KIR2DL3, KIR2DS2 和KIR2DS4）對NK細胞進行染色，使用FITC標記的小鼠 IgG作為對照。沖洗細胞兩次，在流式細胞儀中檢測。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 |
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25344679 | |
| Growth inhibition assay | Cell viability |
|
28717222 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | FTY720 治療使用早期疾病模型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，顯著降低疾病負擔。在所有早期疾病中，F(xiàn)TY720處理的Ph+人類ALL移植瘤降低80±12%。相反, FTY720處理小鼠，與對照組相比，使用四組分開獨立的人類 Ph- ALL 移植瘤，減少白血病發(fā)生率。[3] |
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|---|---|---|
| 動物實驗 | Animal Models | 攜帶ALL細胞的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 |
化學信息&溶解度
| 分子量 | 343.9 | 分子式 | C19H33NO2.HCl |
| CAS號 | 162359-56-0 | SDF | Download Fingolimod (FTY720) HCl SDF |
| Smiles | CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 69 mg/mL ( (200.63 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : 69 mg/mL (200.63 mM) Ethanol : 69 mg/mL (200.63 mM) |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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