Tofacitinib (CP-690550) Citrate

For research use only. Not for use in humans.

Licensed by Pfizer 製品コードS5001 別名:Tasocitinib Citrate

Tofacitinib (CP-690550) Citrate化学構造

CAS No. 540737-29-9

Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity.

サイズ 価格(税別)  
JPY 26400
JPY 80000
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バルク問合せ

文献中Selleckの製品使用例(147)

製品安全説明書

JAK阻害剤の選択性比較

生物活性

製品説明 Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity.
ターゲット
JAK3 [1]
(Cell-free assay)
JAK2 [4]
(Cell-free assay)
1 nM 20 nM
体外試験

Tofacitinib citrate inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. Tofacitinib citrate prevents mixed lymphocyte reaction with IC50 of 87 nM. Tofacitinib citrate treatment of murine factor-dependent cell Patersen–erythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 leads to prevention of cell proliferation with IC50 of 2.1 µM and 0.25 µM, respectively. Tofacitinib citrate inhibits interleukin-6-induced phosphorylation of STAT1 and STAT3 with IC50 of 23 nM and 77 nM, respectively. Moreover, Tofacitinib citrate generates a significant pro-apoptotic effect on murine FDCP-EpoR cells carrying JAK2VV617F, whereas a lesser effect is observed for cells carrying wild-type JAK2. This activity is coupled with the inhibition of phosphorylation of the key JAK2V617F-dependent downstream signaling effectors signal transducer and activator of transcription (STAT)3, STAT5, and v-akt murine thymoma viral oncogene homolog (AKT). [2] Additionally, Tofacitinib citrate prevents IL-15-induced CD69 expression in human and cynomolgus monkey NK and CD8+ T cells in vitro. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Hs578T MoT0SpVv[3Srb36gZZN{[Xl? MYqzJJVO MX2xOkBpenN? MVnJcoR2[3Srb36gc4YhWFSSTk[gbY4hcHWvYX6gTJM2PziWIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JFMhfU1iYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZMhcW5icILld4Vv[2Vib3[gdIVzfmGwYXTheIU> NILlc5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PFEyOid-MkS5O|gyOTJ:L3G+
T-cells M{\VSGZ2dmO2aX;uJIF{e2G7 NYniW5ZWPTBidH:gN|AxKG6P M1PMOlEhcHJ? M1fHeGlvcGmkaYTpc44hd2ZiSlHLNU9LSUt|IHnuJIh2dWGwIFPEOEBxd3OrdHn2[UBVKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWw1NXO2aX31cIF1\WRiU2TBWFYheGixc4Doc5J6dGG2aX;uJIF1KDVyIITvJFMxOCCwTTDwdoVqdmO3YnH0[YQh\m:{IEGgbJIh\m:ubH;3[YQh[nliSVytOEB{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIJ6KGmvbYXuc4Jtd3RiYX7hcJl{cXN? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3MkC2PEc,Ojl6NUKwOlg9N2F-
T-cells MWPGeY5kfGmxbjDhd5NigQ>? MnSxOVAhfG9iM{CwJI5O M1q1clEhcHJ? NH31bmNKdmirYnn0bY9vKG:oIFrBT|EwUkGNMzDpckBpfW2jbjDDSFQheG:|aYTpeoUhXCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOi2|dHnteYxifGWmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBifCCWeYKtOlk2KHKnc3nkeYUh[XRiNUCgeI8hOzByIH7NJJBz\WmwY4XiZZRm\CCob4KgNUBpeiCob3zsc5dm\CCkeTDJUE0zKHO2aX31cIF1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= MkT4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUKwOlgoRjJ7OEWyNFY5RC:jPh?=
T-cells MYjGeY5kfGmxbjDhd5NigQ>? MkTSQlMxOCCwTR?= NET1WZEyKGi{ MmWyTY5pcWKrdHnvckBw\iCMQVuxM2pCUzJxVGnLNkBqdiCqdX3hckBETDRicH;zbZRqfmViVDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmONj3zeIlufWyjdHXkJHNVSVR|IIDoc5NxcG:{eXzheIlwdiCjdDC+N|AxKG6PIIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSCLTD22JJN1cW23bHH0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? M{\KWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWyNFY5Lz5{OUi1NlA3QDxxYU6=
TALL-1 MWnGeY5kfGmxbjDhd5NigQ>? NGT6bXAyKHWP MWmzJIhzew>? NUD6OWVLUW6qaXLpeIlwdiCxZjDKRWs{KGmwIHj1cYFvKFSDTFytNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFnMMVIhcW6mdXPl[EBUXEGWNTDwbI9{eGixconsZZRqd25iYYSgNUB2VSCycnXpcoN2[mG2ZXSg[o9zKDNiaILzJIZwdGyxd3XkJIJ6KEmOLUKgbY5lfWO2aX;uJI1m[XO3cnXkJIFnfGW{IEOwJI1qdnNiYomgbY1ufW6xYnzveJRqdmd? M4TpSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkW4OVIyLz5{NkK1PFUzOTxxYU6=
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OCL-AML5 M2DaPGZ2dmO2aX;uJIF{e2G7 NUTU[mh[OSC3TR?= NF3uT3I{KGi{cx?= NH;IRpZKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hV0OOLVHNUFUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0ZiaX7keYNm\CCVVFHUOUBxcG:|cHjvdplt[XSrb36gZZQhOSC3TTDwdoVqdmO3YnH0[YQh\m:{IEOgbJJ{KG[xbHzve4VlKGK7IFfNMWNUTiCrbnT1Z5Rqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCrbX31co9jdG:2dHnu[y=> NYfFc4FWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yOVg2OjFpPkK2NlU5PTJzPD;hQi=>
BA/F3 NWrQXYhqSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1zkNlczKGi{cx?= NYK4PIhqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKFSHTD3KRWs{KGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzKGeubzDhd5NigQ>? NYD1SIxTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yOVg2OjFpPkK2NlU5PTJzPD;hQi=>
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Huh7 MnvkSpVv[3Srb36gZZN{[Xl? NHjXcWEyOCC3TR?= Ml3DN|AhdWmwcx?= MVPJcohq[mm2aX;uJI9nKFS7a{KgbY4hcHWvYX6gTJVpPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gTWZP[WyyaHG1MYlv\HWlZXSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKGG2IEGwJJVOKHC{ZT3pcoN2[mG2ZXSg[o9zKDNyIH3pcpMh[mWob4LlJGlHVmGucHjhOUB{fGmvdXzheIlwdiCob4KgN|AhdWmwczDtbY5{KGK7IHntcZVvd2Kub4T0bY5o Mmf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{M{GxOVkoRjJ4MkOxNVU6RC:jPh?=
Huh7 MlnwSpVv[3Srb36gZZN{[Xl? NHz2fmQyOCC3TR?= NVzGclY4OzBibXnudy=> NGrRTYxKdmirYnn0bY9vKG:oIGT5b|IhcW5iaIXtZY4hUHWqNzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[mG|YXygcIV3\WxiU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KDFyIIXNJIFnfGW{IEOwJI1qdnNiYomgbY1ufW6xYnzveJRqdmd? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ|MUG1PUc,OjZ{M{GxOVk9N2F-
Huh7 M3zFO2Z2dmO2aX;uJIF{e2G7 MVGxJJVO MWOzNEBucW6| M{DhR2lvcGmkaYTpc44hd2ZiVInrNkBqdiCqdX3hckBJfWh5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBKTk6jbIDoZVUucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25iYYSgNUB2VSCycnWtbY5kfWKjdHXkJIZweiB|MDDtbY5{KGKnZn;y[UBKTk6jbIDoZVUhe3SrbYXsZZRqd25iZn;yJFMxKG2rboOgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? M1nvTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkOxNVU6Lz5{NkKzNVE2QTxxYU6=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
JAK3 / STAT5 / p-STAT5; 

PubMed: 27732937     


The following cell lines: EBV-negative B cell line (BJAB), EBV-transformed lymphoblastoid cell line (LCL), EBV-negative T cell lines (Jurkat and MOLT4), EBV-positive T cell lines (SNT15 and SNT16), EBV-negative NK cell line (KHYG1), and EBV-positive NK cell lines (KAI3 and SNK6), were treated without (−) or with (+) 1 μM tofacitinib for 24 h and cell lysates were then immunoblotted for the indicated proteins.

LMP1 / EBNA1 / BZLF1; 

PubMed: 27732937     


SNT13, SNT15, SNT16, KAI3 and SNK6 cell lines were treated with 5 μM tofacitinib for 48 h, and cell lysates were immunoblotted for LMP1, EBNA1 and BZLF1. Actin was blotted as a loading control.

JAK3 / p-JAK3 / STAT3; 

PubMed: 26082451     


CTCL cell lines were subjected to western blot (tofacitinib 10, 100, 200 nM) (G) after 48 hours of treatment.

27732937 26082451
Growth inhibition assay
Cell number; 

PubMed: 27732937     


BJAB, LCL, Jurkat, SNT15, KHYG1 and KAI3 cells were treated with the indicated concentrations of tofacitinib, and viable cells were counted at the indicated times using the trypan blue exclusion test. Values are means ± SE of the results from triplicate experiments. *P < 0.05 as compared with DMSO-treated cells.

27732937
体内試験 Tofacitinib citrate decrease a delayed-type hyper-sensitivity response and extended cardiac allograft survival in murine models. Furthermore, Tofacitinib citrate treatment of ex-vivo-expanded erythroid progenitors from JAK2V617F-positive PV patients results in specific, antiproliferative (IC50 = 0.2 μM) and pro-apoptotic activity. In contrast, expanded progenitors from healthy controls are less sensitive to Tofacitinib citrate in proliferation (IC50 > 1.0 μM), and apoptosis assays.[2] During 2 weeks of Tofacitinib citrate dosing at 10 and 30 mg/kg/d, a significant, time-dependent decrease in NK cell numbers relative to vehicle treatment is observed. Effector memory CD8+ cell numbers in the Tofacitinib citrate-treated group are 55% less than those observed in animals treated with vehicle.[3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

Enzyme assays:

The JAK1, JAK2, and JAK3 kinase assays utilize a protein expressed in baculovirus-infected SF9 cells (a fusion protein of GST and the catalytic domain of human JAK enzyme) purified by affinity chromatography on glutathione−Sepharose. The substrate for the reaction is polyglutamic acid-tyrosine [PGT (4:1)], coated onto Nunc Maxi Sorp plates at 100 μg/mL overnight at 37 °C. The plates are washed three times, and JAK enzyme is added to the wells, which contained 100 μL of kinase buffer (50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM sodium orthovanadate). For Tofacitinib citrate, it is also added for kinase assay at different doses. After incubation at room temperature for 30 min, the plates are washed three times. The level of phosphorylated tyrosine in a given well is determined by standard ELISA assay utilizing an anti-phosphotyrosine antibody.
細胞試験:

[2]

- 合併
  • 細胞株: FDCP-EpoR JAK2WT and JAK2V617F cell lines
  • 濃度: 0-4 μM
  • 反応時間: 72 hours
  • 実験の流れ:

    Determination of growth inhibition by Tofacitinib citrate is performed using identical culture conditions for both FDCP-EpoR JAK2WT and JAK2V617F cell lines. Briefly, 1 × 105 cells/mL are cultured in 96-well flat-bottom plates at 37 °C in a humidified 5% CO2 atmosphere using RPMI 1640 supplemented with 1.25% FCS, and 5% WEHI supernatant. Decreased FCS concentration is necessary to prevent binding between Tofacitinib citrate and serum proteins. Growth inhibition assays are terminated by addition of 20 μL CellTiter96 One Solution Reagent. Flat-bottom plates are incubated for an additional 3 hours for MTT assay. Absorbance is determined at 595 nm on a BioTek Synergy-HT microplate reader. Results are the average standard deviation of three independent determinations.


    (参考用のみ)
動物試験:

[2]

- 合併
  • 動物モデル: Mauritius-origin adult cynomolgus monkeys
  • 投薬量: 10, 30 mg/kg/d
  • 投与方法: Oral gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (198.21 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
0.5% methylcellulose
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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 504.49
化学式

C16H20N6O.C6H8O7

CAS No. 540737-29-9
Storage powder
in solvent
別名 Tasocitinib Citrate
Smiles CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04496960 Not yet recruiting Drug: tofacitinib|Other: Placebo Sjogren''s Syndrome National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC) January 5 2021 Phase 1|Phase 2
NCT04624230 Not yet recruiting Drug: tofacitinib Ulcerative Colitis Pfizer November 20 2020 Phase 3
NCT04468425 Not yet recruiting Drug: Tofacitinib Citrate Healthy Subjects TWi Biotechnology Inc. November 11 2020 Phase 1
NCT04424303 Not yet recruiting Drug: Tofacitinib Ulcerative Colitis Pfizer September 30 2020 --
NCT04576000 Recruiting Drug: Tofacitinib Ulcerative Colitis Robarts Clinical Trials Inc. August 25 2020 --
NCT04141904 Suspended Drug: Tofacitinib 5 MG [Xeljanz]|Other: Placebo Depression|Inflammation University of Oxford|Wellcome Trust|Medical Research Council February 10 2020 Phase 1|Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What is the difference between the two products (S5001, S2789)?

  • 回答:

    Tofacitinib (S2789) is the base form of Tofacitinib citrate (S5001). The biological activity of these two compound are same. S5001 is better than S2789 for Oral gavage.

JAKシグナル伝達経路

JAK Inhibitors with Unique Features

相関JAK製品

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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