Fingolimod (FTY720) HCl

製品コードS5002

Fingolimod (FTY720) HCl化学構造

分子量(MW):343.9

Fingolimod (FTY720) HCl(フィンゴリモド、Gilenya)は、0.033nMのIC50によるスフィンゴシン1-リン酸(S1P)受容体拮抗剤です。

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カスタマーフィードバック(3)

  •  

     

    Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6  105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6  105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6  105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8).

    Blood 2012 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck.

     

    Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. Id-specific TCR-transgenic and nontransgenic SCID mice were inoculated subcutaneously with 105 MOPC315 myeloma cells embedded in Matrigel.9 TCR-transgenic SCID mice were treated daily with fingolimod (1ug/g bodyweight) or with vehicle only (n=8-10). SCID mice were left untreated (n =2). At day 8, draining lymph nodes and Matrigel plugs were dissected and analyzed by flow cytometry.9 (D) CD69 expression on gated Id-specific CD4 T cells in draining lymph nodes of representative TCR-transgenic SCID mice treated with vehicle only (top) or fingolimod (bottom). Dotted lines indicate an isotype-matched control antibody. (E) Number of Id-specific T cells per Matrigel plug (mean  SEM). (F) Expression of the activation marker MHC class II on Matrigel-infiltrating CD11b macrophages (geometric mean  SEM). P values were calculated with the log-rank test (A-C) and the t test (E-F). ns indicates not significant.

    Blood 2012 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck.

  • FTY720 treatment of ECM decreases lymphocyte numbers and granzyme A mRNA in the brain. (A) Relative CD8+ and (B) CD4+ T-cell numbers isolated from the brains of mice infected for 6 d. Numbers were decreased in animals treated with FTY720 1 d before infection and 1 d p.i. (CD4+: P < 0.5 and P < 0.001, CD8+: P < 0.5 and P < 0.01 respectively, KW and DMC, two pooled IE, n ≥ 4/group/IE) (C) GZMA mRNA levels were decreased in the brains of FTY720-treated animals compared with control animals: for (FTY720 [–1], P < 0.05, FTY720 [+1] P > 0.05 and FTY720 [+3], P < 0.01; KW and DMC, two pooled IE, n ≥ 3/group/IE).

    Mol Med 2011 17, 717- 725 . Fingolimod (FTY720) HCl purchased from Selleck.

製品安全説明書

S1P Receptor阻害剤の選択性比較

生物活性

製品説明 Fingolimod (FTY720) HCl(フィンゴリモド、Gilenya)は、0.033nMのIC50によるスフィンゴシン1-リン酸(S1P)受容体拮抗剤です。
ターゲット
S1P receptor [1]
(K562, NK cells )
0.033 nM
体外試験

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. [1] 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. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U2OS cells MWPGeY5kfGmxbjDhd5NigQ>? MV3B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGOxVFEhemWlZYD0c5Ih\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiY3:t[ZhxemW|c3nu[{BmT0[SIHHzd4V{e2WmIHHzJJJm[2WydH;yJIlvfGW{bnHsbZpifGmxbjDpcpRwKGO7dH;wcIF{dSC3c3nu[{BJd2WlaIP0JIR6\SC|dHHpcolv\yxiRVO1NF0xNjByMjFOwG0v NWLTXGtWOjJzMESxOFQ>
CHO cells MYTGeY5kfGmxbjDhd5NigQ>? NYnyTFBsTGm|cHzhZ4Vu\W62IH;mJHs{O1Cfc4DobY5od3OrbnWgNUBxcG:|cHjheIUh\nKxbTDoeY1idiCVMWCxJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNuIFnDOVA:OC56NDFOwG0v NUHWWlJVOTV4MUW1NVM>
mouse bone marrow cells MlPqR5l1d3SxeHnjxsBie3OjeR?= NH;LWo44OiCq NVn6XIhnS3m2b4TvfIlkcXS7IHHnZYlve3RiQlPSMWFDVCCodYPpc44heHKxdHXpckAyQTBiZYjwdoV{e2mwZzDtc5V{\SCkb37lJI1ienKxdzDj[YxteyCjZoTldkA4OiCqcoOgZpkhfmm2YXyg[JlmKGW6Y3z1d4lwdi:obH;3JIN6fG:vZYTybYMh[W6jbInzbZMtKEmFNUC9N{4{KM7:TT6= NGTTRlgzPDJ5M{[zNi=>
human MCF7 cells M4LmUnBzd2yrZnXyZZRqd25iYYPzZZk> MnnQO|ghcA>? NXL0cItXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFc5KGi{czDifUBYW1RvMTDhd5NigSxiSVO1NF02KM7:TT6= NIHPb3EzOTR3NkWyOC=>
MDA-MB-231 cells MnnaVJJwdGmoZYLheIlwdiCjc4PhfS=> NGDSRYw4QCCq NIXsOoNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{igbJJ{KGK7IGfTWE0yKGG|c3H5MEBKSzVyPTC1JO69VS5? MYWyNVQ2PjV{NB?=
human SK-BR-3 cells Mn[yVJJwdGmoZYLheIlwdiCjc4PhfS=> NHP6[4Q4QCCq NV\hU5hDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd6IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1iNTFOwG0v M2f5XlIyPDV4NUK0
human HCT116 cells Mnr6VJJwdGmoZYLheIlwdiCjc4PhfS=> M{\sflc5KGh? M2TORWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFc5KGi{czDifUBYW1RvMTDhd5NigSxiSVO1NF02KM7:TT6= NYLlPZpNOjF2NU[1NlQ>
human SW620 cells NFm2WJZRem:uaX\ldoF1cW:wIHHzd4F6 MlXxO|ghcA>? MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEe4JIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3ME21JO69VS5? NX62fVJSOjF2NU[1NlQ>
human BLIN-1 cells MXfDfZRwfG:6aXRCpIF{e2G7 MlrCO|IhcA>? M4jnbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCqLX7l[4F1cX[nIHj1cYFvKEKOSV6tNUBk\WyuczDh[pRmeiB5MjDodpMh[nlidnn0ZYwh\HmnIHX4Z4x2e2mxbj;mcI94KGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:PS53IN88UU4> MUKyOFI4OzZ|Mh?=
human BV173 cells NF7DblREgXSxdH;4bYPDqGG|c3H5 MnfoO|IhcA>? M3jifGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCqLYDvd4l1cX[nIHj1cYFvKEKYMUezJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC4aYThcEBlgWViZYjjcJV{cW:wL3\sc5ch[3m2b33leJJq[yCjbnHsfZNqeyxiSVO1NF03NjNizszNMi=> MYGyOFI4OzZ|Mh?=
human DU145 cells MnrNR5l1d3SxeHnjxsBie3OjeR?= MYe3NkBp MmLlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJZqfGGuIHT5[UBmgGOudYPpc44w\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPU[uOUDPxE1w NF;ZUHMzPDJ5M{[zNi=>
human SUP-B15 cells NXPLUIk4S3m2b4TvfIlkyqCjc4PhfS=> NWDyb|NOPzJiaB?= M1;ybWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCqLYDvd4l1cX[nIHj1cYFvKFOXUD3CNVUh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwODFOwG0v NU\0eI5iOjR{N{O2N|I>
human CCRF-CEM cells M2PLVGN6fG:2b4jpZ:Kh[XO|YYm= MY[3NkBp Ml\CR5l1d3SxeHnjbZR6KGGpYXnud5QhWGhvbnXnZZRqfmViaIXtZY4hS0OURj3DSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwODFOwG0v NVrKR3V[OjR{N{O2N|I>
human NALM6 cells M4DTeGN6fG:2b4jpZ:Kh[XO|YYm= MoDJO|IhcA>? NVmz[WpzS3m2b4TvfIlkcXS7IHHnZYlve3RiUHitcoVo[XSrdnWgbJVu[W5iTlHMUVYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7II\peIFtKGS7ZTDlfINtfXOrb36v[oxwfyCleYTvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTlwNjFOwG0v M3ywSlI1Ojd|NkOy
human PC3 cells M{DRTGN6fG:2b4jpZ:Kh[XO|YYm= NF\SS4o4OiCq NHfuXWZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JJZqfGGuIHT5[UBmgGOudYPpc44w\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUmuPEDPxE1w MUSyOFI4OzZ|Mh?=
Sf9 insect cells NF\jVXVHfW6ldHnvckBie3OjeR?= NELZSmMyKGh? M1nRWmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiU{HQUEApPjJidH:gOVY5MSCneIDy[ZN{\WRiaX6gV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCVMWCgZZMhe3Wkc4TyZZRmKGGodHXyJFEhcHJ? MV6yOFgxQThzNB?=
human Jurkat cells M4TSOWZ2dmO2aX;uJIF{e2G7 M1W0eVE5KGh? NHi5SoRT\X[ncoPhcEBw\iCrbnjpZol1cW:wIH;mJI1qfG:laH;u[JJq[WxiZoXuZ5Rqd25iaX6gbJVu[W5iSoXyb4F1KGOnbHzzJIFnfGW{IEG4JIhzeyCrbjDwdoV{\W6lZTDv[kBbNV[DRD3mcYs> NVHqSXFxOTd2MEC1OVU>
mouse MN9D cells NXz5NFFGTnWwY4Tpc44h[XO|YYm= MWOwMlE3KM7:TR?= NELSNno4OiCq MUXO[ZVzd3C{b4TlZ5RqfmViYXP0bZZqfHliaX6gcY92e2ViTV65SEBk\WyuczDhd5Nme3OnZDDhd{BjdG:la3nu[{Bw\iCWTl[tZYxxcGFiYYPzc4Nq[XSnZDD0c5hq[2m2eTDheEAxNjF4IIXNJIFnfGW{IEeyJIhzeyCkeTDUdplx[W5iYnz1[UB{fGGrbnnu[{4> MX6yOVA2ODF4NR?=
mouse MN9D cells M2fFfWZ2dmO2aX;uJIF{e2G7 NWH6UIhrOC5zNjFOwG0> NUH5VVZTOjRiaB?= M2i1Sm5mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDpckBud3W|ZTDNUllFKGOnbHzzJIF{e2W|c3XkJIF{KHO2aX31cIF1cW:wIH;mJGJFVkZiZYjwdoV{e2mxbjDheEAxNjF4IIXNJIFnfGW{IEK0JIhzew>? MUKyOVA2ODF4NR?=
rat PC12 cells MXfGeY5kfGmxbjDhd5NigQ>? NVzueFU1PSEQvF2= MYmzNEB1dyBzMkCgcYlvew>? MV3JcoR2[3Srb36gc4YhWFB{QTDjZZRidHm2aXOgd5VjfW6rdDDhZ5Rqfmm2eTDpckBz[XRiUFOxNkBk\WyuczDhd5Nme3OnZDDhd{BxcG:|cHjheIUhdGW4ZXygZZQhPSC3TTDt[YF{fXKnZDCzNEB1dyBzMkCgcYlvey5? Mle0NlUxPTBzNkW=
mouse MN9D cells NIfCSohHfW6ldHnvckBie3OjeR?= MYO1JO69VQ>? M3ntOmlv\HWldHnvckBw\iCSUELBJINifGGueYTpZ{B{fWK3bnn0JIFkfGm4aYT5JIlvKG2xdYPlJG1PQURiY3XscJMh[XO|ZYPz[YQh[XNicHjvd5Bp[XSnIHzleoVtKGG2IEWgeW0> NImzU2czPTB3MEG2OS=>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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. [3]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
+ 展開
  • 細胞株: Immature DCs
  • 濃度: 10 nM
  • 反応時間: 4 hours
  • 実験の流れ: Immature DCs are left intact or are incubated with 2 μM S1P, 10 nM FTY720, 10 nM SEW2871 or the combinations of S1P with these drugs for 4 hours. As a control 1 μg/mL LPS is used. The cells are washed and incubated in a 96-well plate (v-bottom, 2 × 105 cells per well), washed again and resuspended in PBS buffer containing 0.1% sodium azide. They are labeled with 1 μg/mL FITC-conjugated mouse anti-human CD80, 1 μg/mL FITC-conjugated mouse anti-human CD83, 1 μg/mL FITC-conjugated mouse anti-human CD86, 1 μg/mL FITC-conjugated mouse anti-human HLA-class I, 1 μg/mL FITC-conjugated mouse anti-human HLA-DR, 1 μg/mL FITC-conjugated mouse anti-human HLA-E, or 1 μg/mL FITC-conjugated mouse IgG as a control. The cells are washed twice, and examined in the flow cytometer. Markers are set according to the isotype control FITC-conjugated mouse IgG. To stain NK cells with antibodies for various NK cell activating receptors, they are either left untreated or incubated with 2 μM S1P for 4 hours, washed and stained with 1 μg/mL PE-conjugated mouse anti-human NKp30 (CD337), 1 μg/mL PE-conjugated mouse anti-human NKp44 (CD336), 1 μg/mL PE-conjugated mouse anti-human NKG2D (CD314), or as a control 1 μg/mL PE-conjugated mouse IgG1, for 45 min at 4 °C. NK cells are also stained with 1 μg/mL FITC-conjugated anti-killer inhibitory receptor (KIR)/CD158 antibody which recognizes KIR2DL2, KIR2DL3, KIR2DS2 and KIR2DS4, and as a control with FITC-conjugated mouse IgG. The cells are washed twice, and examined in the flow cytometer. Markers are set according to the isotype control PE-conjugated or FITC-conjugated mouse IgG.
    (参考用のみ)
動物試験:[3]
+ 展開
  • 動物モデル: NOD/SCIDγc−/− mice bearing ALL cells.
  • 製剤: 2% ethanol or saline
  • 投薬量: 5 mg/kg/day, 10 mg/kg/day
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 69 mg/mL (200.63 mM)
Water 69 mg/mL (200.63 mM)
Ethanol 69 mg/mL (200.63 mM)
体内 順序で溶剤を入れること:
Saline
20 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 343.9
化学式

C19H33NO2.HCl

CAS No. 162359-56-0
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01633112 Active, not recruiting Relapsing-remitting Multiple Sclerosis (RRMS) Novartis Pharmaceuticals|Novartis August 9, 2012 Phase 4
NCT02956200 Not yet recruiting Stroke|Inflammation Second Affiliated Hospital, School of Medicine, Zhejiang University November 2016 Phase 2
NCT02575365 Recruiting Cognition|Brain Volume Loss Novartis Pharmaceuticals|Novartis February 2016 Phase 4
NCT02490930 Recruiting Glioblastoma|Anaplastic Astrocytoma Sidney Kimmel Comprehensive Cancer Center July 2015 Early Phase 1
NCT02939079 Completed Multiple Sclerosis Isfahan University of Medical Sciences|Shiraz University of Medical Sciences April 2015 Phase 2|Phase 3
NCT02373098 Recruiting Relapsing Remitting Multiple Sclerosis Novartis Pharmaceuticals|Novartis March 2015 Phase 4

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

S1P Receptor信号経路図

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID