1. MAPK/ERK Pathway
  2. JNK
  3. Tanzisertib

Tanzisertib  (Synonyms: CC-930)

目录号: HY-15495 纯度: 99.87%
COA 产品使用指南

Tanzisertib (CC-930) 是有效的 JNK1/2/3 抑制剂,IC50 分别为61/7/6 nM。

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Tanzisertib Chemical Structure

Tanzisertib Chemical Structure

CAS No. : 899805-25-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥990
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1 mg ¥454
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5 mg ¥1000
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10 mg ¥1650
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50 mg ¥6600
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200 mg   询价  

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Top Publications Citing Use of Products

    Tanzisertib purchased from MCE. Usage Cited in: Nat Cell Biol. 2017 Jun;19(6):698-710.  [Abstract]

    Immunoblot analysis of phospho-JNK of splenic XBP1ΔDC CD11c+ cells of XBP1ΔDC mice treated with CC-930 or vehicle. Total JNK and β-tubulin levels serve as loading control. Each lane represents one mouse.

    查看 JNK 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively.

    IC50 & Target[1]

    JNK3

    6 nM (IC50)

    JNK2

    7 nM (IC50)

    JNK1

    61 nM (IC50)

    体外研究
    (In Vitro)

    Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM)[1]. Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes[2]. Tanzisertib (CC-930) blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis[3].

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

    体内研究
    (In Vivo)

    Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model[1]. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis[3].

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

    Clinical Trial
    分子量

    448.44

    Formula

    C21H23F3N6O2

    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    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: 

    1M HCl 中的溶解度 : 100 mg/mL (223.00 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

    DMSO 中的溶解度 : ≥ 33 mg/mL (73.59 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2300 mL 11.1498 mL 22.2995 mL
    5 mM 0.4460 mL 2.2300 mL 4.4599 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。

    • 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 (5.57 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。

      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 (5.57 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。

      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。
    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

    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: 99.87%

    参考文献
    Cell Assay
    [3]

    Systemic sclerosis (SSc) fibroblasts are incubated with 1 µM Tanzisertib (CC-930) in 96-well plates for 20 h. Then MTT is added at a final concentration of 1 mg/mL, and the cells are further incubated at 37°C for 4 h. Mock-treated fibroblasts are used as controls, and all other results are normalised to untreated cells.

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

    Animal Administration
    [3]

    To evaluate the regression of fibrosis on inhibition of JNK, a modified model of bleomycin-induced dermal fibrosis is used. In this model, treatment is initiated 3 weeks after the beginning of the challenge with bleomycin, when significant dermal fibrosis is already established. The outcome of six different groups with a total number of 40 mice is analysed. The first group of mice receive subcutaneous injections of NaCl for 6 weeks. The second group is injected for 3 weeks with bleomycin followed by injections of NaCl for another 3 weeks to analyse the degree of fibrosis before treatment, and to control the spontaneous regression of fibrosis. The third group of mice is killed after 6 weeks of injections with bleomycin. The fourth and the fifth group are treated with Tanzisertib (CC-930) at doses of 50 mg/kg and 150 mg/kg for the last 3 weeks of continuous challenge with bleomycin for 6 weeks. The sixth group is a positive control group consisting of mice challenged with bleomycin for 6 weeks and treated in parallel with imatinib at doses of 50 mg/kg for the last 3 weeks.

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

    参考文献

    Tanzisertib 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
    DMSO / 1M HCl 1 mM 2.2300 mL 11.1498 mL 22.2995 mL 55.7488 mL
    5 mM 0.4460 mL 2.2300 mL 4.4599 mL 11.1498 mL
    10 mM 0.2230 mL 1.1150 mL 2.2300 mL 5.5749 mL
    15 mM 0.1487 mL 0.7433 mL 1.4866 mL 3.7166 mL
    20 mM 0.1115 mL 0.5575 mL 1.1150 mL 2.7874 mL
    25 mM 0.0892 mL 0.4460 mL 0.8920 mL 2.2300 mL
    30 mM 0.0743 mL 0.3717 mL 0.7433 mL 1.8583 mL
    40 mM 0.0557 mL 0.2787 mL 0.5575 mL 1.3937 mL
    50 mM 0.0446 mL 0.2230 mL 0.4460 mL 1.1150 mL
    60 mM 0.0372 mL 0.1858 mL 0.3717 mL 0.9291 mL
    1M HCl 80 mM 0.0279 mL 0.1394 mL 0.2787 mL 0.6969 mL
    100 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5575 mL
    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.

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    目录号:
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