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Tofacitinib (CP-690550) Citrate

別名：Tasocitinib Citrate,CP-690550

トファシチニブクエン酸塩 (Tofacitinib citrate (CP-690550、タソシチニブ)) は JAK の新規阻害剤です。IC50は JAK3, JAK2, JAK1 に対してそれぞれ 1 nM, 20 nM, 112 nM です。 トファシチニブクエン酸塩は抗感染作用を持ちます。

Tofacitinib (CP-690550) Citrate化学構造

CAS No. 540737-29-9

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 70500 国内在庫あり
JPY 100500 国内在庫なし(納期7~10日)
JPY 235500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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製品安全説明書

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Tofacitinib (CP-690550) Citrate関連製品

シグナル伝達経路

JAK Signaling Pathways

JAKシグナル伝達経路

JAK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
NK Immunosuppressive assay 1 to 5 mg/kg 4 weeks Immunosuppressive activity in naive cynomolgus monkey assessed as effect on CD3-CD16+ NK cells at 1 to 5 mg/kg, po for 4 weeks 14593182
T-cells Function assay 5 to 500 nM 1 hr Inhibition of IL2-induced Stat5 phosphorylation in human CD4+ T cells at 5 to 500 nM after 1 hr by Western blot 19053756
SUM149PT Function assay 3 uM 16 hrs Induction of PTPN6 in human SUM149PT cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate 24978112
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生物活性

製品説明 トファシチニブクエン酸塩 (Tofacitinib citrate (CP-690550、タソシチニブ)) は JAK の新規阻害剤です。IC50は JAK3, JAK2, JAK1 に対してそれぞれ 1 nM, 20 nM, 112 nM です。 トファシチニブクエン酸塩は抗感染作用を持ちます。
Targets
JAK3 [1]
(Cell-free assay)		 JAK2 [4]
(Cell-free assay)
1 nM 20 nM
In Vitro
In vitro 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]
Kinase Assay 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.
細胞実験 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot JAK3 / p-JAK3 / STAT3 LMP1 / EBNA1 / BZLF1 JAK3 / STAT5 / p-STAT5 26082451
Growth inhibition assay Cell number 27732937
In Vivo
In Vivo 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]
動物実験 動物モデル Mauritius-origin adult cynomolgus monkeys
投与量 10, 30 mg/kg/d
投与経路 Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06202560 Enrolling by invitation
Frontal Fibrosing Alopecia|Lichen Planopilaris
Institute of Dermatology Thailand
 November 29 2023 Not Applicable
NCT05487703 Completed
Arthritis Rheumatoid
Pfizer
 November 14 2022 --
NCT05082428 Completed
Ulcerative Colitis
Pfizer
 May 30 2022 --
NCT05728008 Completed
Ulcerative Colitis
IRCCS San Raffaele
 April 5 2022 --
NCT04768504 Recruiting
Immune-Mediated Colitis
Khashayar Esfahani|Sir Mortimer B. Davis - Jewish General Hospital
 March 22 2022 Phase 2

化学情報

分子量 504.49 化学式

C16H20N6O.C6H8O7
CAS No. 540737-29-9 SDF Download Tofacitinib (CP-690550) Citrate SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (198.21 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機
Clear solution
5%DMSO 95% Corn oil
2.5mg/ml (4.96mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(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）

mg/kg g μL 匹

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
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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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.

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