2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. JAK Apoptosis
  4. Tofacitinib

Tofacitinib  (Synonyms: 托法替尼; Tasocitinib; CP-690550)

目录号: HY-40354 纯度: 99.94%
COA 产品使用指南

摩尔计算器

Tofacitinib是 JAK3/2/1 抑制剂，IC50 分别为1，20 和 112 nM。

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Tofacitinib Chemical Structure

Tofacitinib Chemical Structure

CAS No. : 477600-75-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥375
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10 mg ￥600
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50 mg ￥1500
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100 mg ￥2500
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200 mg ￥3500
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500 mg ￥6500
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1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Tofacitinib:

Tofacitinib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 48 篇科研文献

IP

    Tofacitinib purchased from MCE. Usage Cited in: Pulm Pharmacol Ther. 2017 Apr;43:60-67.  [Abstract]

    Effect of Tofacitinib administered 1 h before LPS challenge. (A) Effect of different doses of Tofacitinib on STAT3 activation in lung homogenates obtained 30 min after LPS challenge. (B) Effect of different doses of Tofacitinib on STAT3 activation in lung homogenates obtained 4 h after LPS challenge.

    查看 JAK 亚型特异性产品:

    查看所有亚型
    JAK1 JAK2 JAK3 Tyk2 JAK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

    IC50 & Target[1]

    JAK3

    1 nM (IC50)

    JAK2

    20 nM (IC50)

    JAK1

    112 nM (IC50)

    Rock-II

    3400 nM (IC50)

    Lck

    3870 nM (IC50)

    体外研究
    (In Vitro)

    Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (Kd). The report includes additional binding for Tofacitinib at Camk1 (Kd of 5,000 nM), DCamkL3 (Kd of 4.5 nM), Mst2 (Kd of 4,300 nM), Pkn1 (Kd of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (Kd of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (Kd of 1,200 nM), Snark (Kd of 420 nM), Tnk1 (Kd of 640 nM) and Tyk2 (Kd of 620 nM)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Tofacitinib 相关抗体:
    体内研究
    (In Vivo)

    Animals that are treated with Tofacitinib show a significantly lower production of anti-drug antibodies (ADAs) compare with PEG-treated control mice (for five weeks after initial immunization, p<0.01, n=8). Moreover ADAs become detectable earliest on day 28. A difference of 1000- to 200-fold in titers to SS1P is apparent from days 21 through 35, respectively. Compare to SS1P, mice injected with keyhole limpet hemocyanin (KLH) generate a more rapid antibody response. Yet, the administration of Tofacitinib reduces anti-KLH titers compare to controls (p<0.05 on day 21, p<0.01 on day 28, respectively, n=5). Reductions in titers ranged from 5000- to 250-fold from days 21 through 28, respectively[2]. Based on previous dose-response studies, a daily dose of Tofacitinib of 6.2 mg/kg is selected to provide 80% inhibition of hind paw volume and plasma exposure capable of suppressing the JAK1 and JAK3 signaling pathways for >4 hours[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    312.37

    Formula

    C16H20N6O
    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    中文名称

    托法替尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (400.17 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 2.5 mg/mL (8.00 mM; 超声助溶)

    H2O 中的溶解度 : 0.15 mg/mL (0.48 mM; 超声加热助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.2013 mL 16.0067 mL 32.0133 mL
    5 mM 0.6403 mL 3.2013 mL 6.4027 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (8.00 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.00 mM); 澄清溶液

    以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 0.5% MC  0.5% Tween-80

      Solubility: 5 mg/mL (16.01 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.99%

    COA (197 KB) HNMR (199 KB) LCMS (99 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    Kinase activity is recorded via a competition binding assay of selected kinases that are fused to a proprietary tag. Measurements of the amount of kinase binds to an immobilized, active-site directed ligand in the presence and absence of the test compound (e.g., Tofacitinib) provide a % of DMSO control for binding of ligand. Activities between 0 and 10 are selected for Kd determinations. Dendrogram representations are generated by an in-house visualization tool designated PhyloChem[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Human CD4+ positive cells are enriched from peripheral blood mononuclear cells obtained from a healthy donor by magnetic separation (CD4+ MACS beads). CD4+ cells are activated for 3 days with plate bound anti-CD3 and anti CD28 antibodies (5 ug/mL each), and then expanded for another 4 days in the presence of IL-2 (50 U/mL). Cells are rested overnight in 1% RPMI, and pre-incubated with Tofacitinib or DMSO control for 1 hour at indicated concentrations (5 nM, 50 nM, 500 nM; DMSO concentration is equal in all preparations) and then activated with IL-2 (1000 u/mL) or IL-12 (100 ng/mL) for 15 minutes. Cells (10×106/condition) are lysed in 1% Triton-x lysis buffer and equal amounts of cell lysate are run in NuPage Bis-Tris gel (4-12% gradient). Proteins are transferred onto nitrocellulose membrane. Detection is done with indicated antibodies using Odyssey western blotting system[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2][3]

    Mice[2]
    Female BALB/c mice (6-8 weeks old) are used. Mice receive Tofacitinib in PEG300 (100 mg/mL) or vehicle alone (PEG300) by osmotic pump infusion (Alzet Model 2004, 0.25 μL/hour, 28 days). Four days prior to immunization, mice are anesthetized and their dorsal surface is shaved. A one cm incision is made on the back to create a subcutaneous pocket and insert the pump. The incision site is closed with wound clips. Mice are injected weekly (i.p.) with SS1P recombinant immunotoxin (RIT; 5 μg/mouse) beginning on day 0; control mice received injections of saline alone. Every week before SS1P or vehicle immunization, 50 μL of blood is drawn to obtain serum samples. Sera are stored at −80°C until analyzed.
    Rats[3]
    Adjuvant-induced arthritis (AIA) is induced in female Lewis rats. Rats are randomized according to hind paw volume and assigned to Tofacitinib or vehicle treatment regimens. Groups of 7-8 rats per treatment group, and normal naive rats (n=4 per group), are euthanized either 4 hours, 4 days, or 7 days after beginning treatment (days 16, 20, and 23 after immunization, respectively). Tofacitinib is suspended in 0.5% methylcellulose/0.025% Tween 20 for in vivo studies. Once-daily oral administration of vehicle or Tofacitinib (6.2 mg/kg) is initiated on day 16 following immunization and continued through day 23. Paw volumes are reassessed 4 and 7 days after the beginning of treatment (days 20 and 23 after immunization, respectively). For micro-computed tomography (micro-CT) imaging, as well as tartrate-resistant acid phosphatase (TRAP) staining in paw tissue, AIA is induced in a separate cohort of Lewis rats.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Tofacitinib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 3.2013 mL 16.0067 mL 32.0133 mL 80.0333 mL
    5 mM 0.6403 mL 3.2013 mL 6.4027 mL 16.0067 mL
    DMSO 10 mM 0.3201 mL 1.6007 mL 3.2013 mL 8.0033 mL
    15 mM 0.2134 mL 1.0671 mL 2.1342 mL 5.3356 mL
    20 mM 0.1601 mL 0.8003 mL 1.6007 mL 4.0017 mL
    25 mM 0.1281 mL 0.6403 mL 1.2805 mL 3.2013 mL
    30 mM 0.1067 mL 0.5336 mL 1.0671 mL 2.6678 mL
    40 mM 0.0800 mL 0.4002 mL 0.8003 mL 2.0008 mL
    50 mM 0.0640 mL 0.3201 mL 0.6403 mL 1.6007 mL
    60 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3339 mL
    80 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0004 mL
    100 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tofacitinib477600-75-2Tasocitinib CP-690550托法替尼CP690550CP 690550CP-690550JAKApoptosisJanus kinaseInhibitorinhibitorinhibit

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