2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis Anti-infection
  3. JAK Apoptosis Bacterial Fungal Influenza Virus
  4. Tofacitinib citrate

Tofacitinib citrate  (Synonyms: 枸橼酸托法替尼; Tasocitinib citrate; CP-690550 citrate)

目录号: HY-40354A 纯度: 99.98%
COA 产品使用指南

摩尔计算器

Tofacitinib citrate是 JAK3/2/1 抑制剂，IC50 分别为1，20 和 112 nM。Tofacitinib citrate 具有抗菌，抗真菌和抗病毒活性。

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Tofacitinib citrate Chemical Structure

Tofacitinib citrate Chemical Structure

CAS No. : 540737-29-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
1 mg ￥187
In-stock
5 mg ￥375
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10 mg ￥600
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50 mg ￥1500
In-stock
100 mg ￥2500
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200 mg ￥4250
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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 citrate:

Tofacitinib citrate 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 citrate 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 citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

    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].
    K562, KCL22, and THP-1 cells are exposed to different doses of STI571 or JAK inhibitors for 72 h to quantify the effects of tyrosine kinase inhibitor (TKI) activity. Cell growth inhibition is then evaluated using the MTT assay. The proliferation of K562 and KCL22 cells, but not THP-1 cells, is inhibited by IMA in a concentration-dependent manner. The IC50 value of IMA is 0.28 μM for K562 and 0.17 μM for KCL22. Although treatment with Tofacitinib (TOF) or INCB018424 alone does not suppress cell proliferation, both Tofacitinib and INCB018424 make the K562 and KCL22 more sensitive to IMA[4].

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

    Tofacitinib citrate 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

    504.49

    Formula

    C22H28N6O8
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    枸橼酸托法替尼；枸橼酸托法替布
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 28.57 mg/mL (56.63 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)

    H2O 中的溶解度 : 3.33 mg/mL (6.60 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9822 mL 9.9110 mL 19.8220 mL
    5 mM 0.3964 mL 1.9822 mL 3.9644 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 (sealed storage, away from moisture and light)。-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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.96 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.96 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    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： 50% PEG300    50% Saline

      Solubility: 2.5 mg/mL (4.96 mM); 澄清溶液; 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）。

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

    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: 99.98%

    COA (177 KB) RP-HPLC (170 KB) 元素分析报告 (216 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [4]

    Cell survival assay is performed using MTT. Briefly, K562, KCL22, and THP-1 cells (1×105 cells/well) are plated onto 96-well microplates and treated with or without IMA (0.06-1.0 μM) and/or Tofacitinib (10-1,000 nM) or RUX (10-1,000 nM) for 72 h at 37°C in a humidified 5% (v/v) CO2 atmosphere. The medium (200 µL) is then incubated with 10 µL of 5 mg/ml MTT solution for 4 h at 37°C. After being centrifuged at 352 g for 5 min, the culture medium is removed, and 100 µL of DMSO are added to each well to dissolve the formazan. Absorbance is measured at 570 nm using a microplate reader. The results are expressed as percentages[4].

    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 (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). 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 citrate 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 (sealed storage, away from moisture and light)。-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
    H2O / DMSO 1 mM 1.9822 mL 9.9110 mL 19.8220 mL 49.5550 mL
    5 mM 0.3964 mL 1.9822 mL 3.9644 mL 9.9110 mL
    DMSO 10 mM 0.1982 mL 0.9911 mL 1.9822 mL 4.9555 mL
    15 mM 0.1321 mL 0.6607 mL 1.3215 mL 3.3037 mL
    20 mM 0.0991 mL 0.4955 mL 0.9911 mL 2.4777 mL
    25 mM 0.0793 mL 0.3964 mL 0.7929 mL 1.9822 mL
    30 mM 0.0661 mL 0.3304 mL 0.6607 mL 1.6518 mL
    40 mM 0.0496 mL 0.2478 mL 0.4955 mL 1.2389 mL
    50 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9911 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:

    Tofacitinib540737-29-9TasocitinibCP-690550枸橼酸托法替尼枸橼酸托法替布CP690550CP 690550JAKApoptosisBacterialFungalInfluenza VirusJanus kinaseInhibitorinhibitorinhibit

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