1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. VX-11e

VX-11e 是一种高效的,具有选择性的,可口服的 ERK 抑制剂,Ki 值 < 2 nM。

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VX-11e Chemical Structure

VX-11e Chemical Structure

CAS No. : 896720-20-0

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥941
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1 mg ¥388
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5 mg ¥855
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10 mg ¥1305
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25 mg ¥2610
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50 mg ¥3720
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100 mg ¥5940
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of VX-11e:

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Top Publications Citing Use of Products

    VX-11e purchased from MCE. Usage Cited in: J Prac Med. 2016, 32 (11): 1734-1737.

    Signaling pathways analysis of effects of BSP on RAW264.7 cells proliferation.

    VX-11e purchased from MCE. Usage Cited in: Oncotarget. 2016 Apr 26;7(17):23300-11.  [Abstract]

    A. HNSCC cells are treated with DMSO vehicle or VX-11e (0.5 μM) for 24 h and cell protein extracts analyzed. VX-11e inhibits phosphorylation of RSK1 in Cal33 and HSC-6. B. VX-11e inhibits phosphorylation of RSK1 in FaDu engineered cells.

    查看 ERK 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

    VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.

    IC50 & Target[1]

    ERK2

    2 nM (Ki)

    GSK3

    395 (Ki)

    AURA

    540 (Ki)

    CDK2

    852 (Ki)

    体外研究
    (In Vitro)

    VX-11e 在 HT29 细胞增殖试验中具有活性 (IC50=48 nM)[1]

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

    体内研究
    (In Vivo)

    VX-11e 在大鼠和小鼠中均具有口服生物利用度[1]。VX-11e (50 mg/kg,po) 强烈抑制 pRSK,并抑制携带人黑色素瘤 RPDX 肿瘤的 NSG 小鼠的肿瘤生长。VX-11e 与 BKM120 显著改善肿瘤生长抑制[2]

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

    分子量

    500.35

    Formula

    C24H20Cl2FN5O2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 : ≥ 100 mg/mL (199.86 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 1.9986 mL 9.9930 mL 19.9860 mL
    5 mM 0.3997 mL 1.9986 mL 3.9972 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: ≥ 3.25 mg/mL (6.50 mM); 澄清溶液

      此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 32.5 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% Corn Oil

      Solubility: ≥ 3.25 mg/mL (6.50 mM); 澄清溶液

      此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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: 99.17%

    参考文献
    Kinase Assay
    [1]

    Compounds are assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) is incubated with various concentrations of the compounds in DMSO (2.5%) for 10 min. at 30°C in 0.1 mol/L HEPES buffer, pH=7.5, containing 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase and 200 μM erktide peptide. The reaction is initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM is monitored.

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

    Cell Assay
    [1]

    Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter.

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

    Animal Administration
    [2]

    Human melanoma RPDX tumors are expanded in vivo using NSG mice prior to the therapy experiments. Pooled tumor chunks banked from early mouse passages are implanted into 50 NSG mice (1:10 expansion). These tumors are harvested when reaching the maximum volume allowed on the protocol (1,000 mm3), digested, and banked as live cells. The larger part of this stock is retained as a master bank, and the other part is implanted at a 1:5 ratio into NSG mice to use in the therapy experiments. The expansion phase is under continuous drug pressure with PLX4720 200 ppm chemical additive diet at approximately clinical plasma levels. The plasma levels of PLX4720 (103.7 μg/mL ±3.2 after 7 days) are similar to steady-state levels in patients treated with vemurafenib 960 mg twice a day (130.6 μg/mL±71.78). When tumors have reached 200 mm3 per caliper measurement, animals are randomized into treatment groups followed by a 3-day ishout phase. Tumor size is assessed twice weekly per caliper measurement. Mice are sacrificed after two weeks of treatment or when necessary for animal welfare. Dosing is prolonged when tumor control is achieved as indicated. Tumor tissue is conserved in formalin (for FFPE) and snap-frozen in liquid N2 for protein extraction. Treatment groups are sacrificed 4 hours after last dose.

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

    参考文献

    VX-11e 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 1 mM 1.9986 mL 9.9930 mL 19.9860 mL 49.9650 mL
    5 mM 0.3997 mL 1.9986 mL 3.9972 mL 9.9930 mL
    10 mM 0.1999 mL 0.9993 mL 1.9986 mL 4.9965 mL
    15 mM 0.1332 mL 0.6662 mL 1.3324 mL 3.3310 mL
    20 mM 0.0999 mL 0.4997 mL 0.9993 mL 2.4983 mL
    25 mM 0.0799 mL 0.3997 mL 0.7994 mL 1.9986 mL
    30 mM 0.0666 mL 0.3331 mL 0.6662 mL 1.6655 mL
    40 mM 0.0500 mL 0.2498 mL 0.4997 mL 1.2491 mL
    50 mM 0.0400 mL 0.1999 mL 0.3997 mL 0.9993 mL
    60 mM 0.0333 mL 0.1666 mL 0.3331 mL 0.8328 mL
    80 mM 0.0250 mL 0.1249 mL 0.2498 mL 0.6246 mL
    100 mM 0.0200 mL 0.0999 mL 0.1999 mL 0.4997 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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    产品名称:
    VX-11e
    目录号:
    HY-14178
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