2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK Apoptosis
  3. Aurora Kinase FLT3 VEGFR FGFR Src PDGFR Apoptosis
  4. ENMD-2076 Tartrate

ENMD-2076 Tartrate 

目录号: HY-10987 纯度: 99.41%
COA 产品使用指南

摩尔计算器

ENMD-2076 Tartrate 是多靶点激酶抑制剂，抑制 Aurora A，Flt3，KDR/VEGFR2，Flt4/VEGFR3，FGFR1，FGFR2，Src，PDGFRα 的IC50 值分别为1.86，14，58.2，15.9，92.7，70.8，20.2 and 56.4 nM。

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ENMD-2076 Tartrate Chemical Structure

ENMD-2076 Tartrate Chemical Structure

CAS No. : 1453868-32-0

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1390
In-stock
5 mg ￥1200
In-stock
10 mg ￥1800
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of ENMD-2076 Tartrate:

ENMD-2076 Tartrate 相关抗体

Top Publications Citing Use of Products

    ENMD-2076 Tartrate purchased from MCE. Usage Cited in: Int J Gynecol Cancer. 2017 Oct;27(8):1666-1674.  [Abstract]

    Enhanced cytotoxicity in OCCC cells treated with ENMD-2076 plus Cisplatin. Western blot analysis showing that phospho-Aurora-A protein levels are decreased at 0.5-12 hours after treatment with ENMD-2076.

    查看 Aurora Kinase 亚型特异性产品:

    查看所有亚型
    Aurora Kinase Aurora A Aurora B Aurora C

    查看 VEGFR 亚型特异性产品:

    查看所有亚型
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    查看 FGFR 亚型特异性产品:

    查看所有亚型
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    查看 Src 亚型特异性产品:

    查看所有亚型
    Lck Fyn Blk

    查看 PDGFR 亚型特异性产品:

    查看所有亚型
    PDGFR PDGFRβ PDGFRα

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

    IC50 & Target[1]

    Aurora A

    1.86 nM (IC50)

    KDR

    58.2 nM (IC50)

    Flt-4

    15.9 nM (IC50)

    FGFR1

    92.7 nM (IC50)

    FGFR2

    70.8 nM (IC50)

    PDGFRα

    56.4 nM (IC50)

    Flt3

    14 nM (IC50)

    体外研究
    (In Vitro)

    ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 nM[1].

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

    ENMD-2076 Tartrate 相关抗体:
    体内研究
    (In Vivo)

    ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[1].

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

    525.56

    Formula

    C25H31N7O6
    CAS 号
    性状

    固体

    颜色

    Light brown to khaki

    运输条件

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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 25 mg/mL (47.57 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9027 mL 9.5137 mL 19.0273 mL
    5 mM 0.3805 mL 1.9027 mL 3.8055 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 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

    动物实验：

    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: ≥ 1.43 mg/mL (2.72 mM); 澄清溶液

      此方案可获得 ≥ 1.43 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 14.3 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: ≥ 1.43 mg/mL (2.72 mM); 澄清溶液

      此方案可获得 ≥ 1.43 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 14.3 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。

      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

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.42%

    COA (267 KB) LCMS (267 KB)

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

    Recombinant Aurora A and B kinase enzymes assays are carried out in kinase assay buffer (50 mM of HEPES, pH 7.5, 10 mM of MgCl2, 5 mM of EGTA, 0.05% Brij-35) supplemented with 2 mM of DTT. Activities are determined at an ATP concentration equivalent to the apparent Km for each enzyme, and an enzyme concentration that results in approximately 30% phosphorylation of the peptide substrate after 1 hour. Dose–response curves of relative enzyme activity versus ENMD-2076 concentration are plotted with Grafit and used to calculate IC50 values[1].

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

    The antiproliferative effect of ENMD-2076 on adherent tumor cell lines is measured by plating 500 cells per well in a 96-well plate and incubating with 9 doses of compound, spanning 0.3 nM to 125 mM, for 96 hours. Cellular proliferation is measured using the sulforhodamine B assay[1].

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

    Mice: Cell lines are injected subcutaneously or into the mammary fat pad (MDA-MB-231 only) of 5- to 6-week-old CB.17 SCID or NCr nude mice. Tumors are allowed to grow for 10 to 50 days before drug treatment. All treatments are with ENMD-2076 in water or ENMD-2076 free base in CMC-Tween vehicle (0.075% carboxymethylcellulose, 0.085% Tween 80 in water), administered orally. Percent tumor growth inhibition is calculated[1].

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

    ENMD-2076 Tartrate 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9027 mL 9.5137 mL 19.0273 mL 47.5683 mL
    5 mM 0.3805 mL 1.9027 mL 3.8055 mL 9.5137 mL
    10 mM 0.1903 mL 0.9514 mL 1.9027 mL 4.7568 mL
    15 mM 0.1268 mL 0.6342 mL 1.2685 mL 3.1712 mL
    20 mM 0.0951 mL 0.4757 mL 0.9514 mL 2.3784 mL
    25 mM 0.0761 mL 0.3805 mL 0.7611 mL 1.9027 mL
    30 mM 0.0634 mL 0.3171 mL 0.6342 mL 1.5856 mL
    40 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 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.

    Keywords:

    ENMD-20761453868-32-0ENMD2076ENMD 2076Aurora KinaseFLT3VEGFRFGFRSrcPDGFRApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Vascular endothelial growth factor receptorFibroblast growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

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    目录号：
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