2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Ki8751

Ki8751是有效地 VEGFR2 抑制剂，IC50 值为0.9 nM。

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Ki8751 Chemical Structure

Ki8751 Chemical Structure

CAS No. : 228559-41-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥522
In-stock
5 mg ￥505
In-stock
10 mg ￥884
In-stock
50 mg ￥2727
In-stock
100 mg ￥4725
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Ki8751 相关抗体

Top Publications Citing Use of Products

    Ki8751 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):982.  [Abstract]

    Western blot is performed to detect the expression of VEGFR2, p-VEGFR2, Akt, p-Akt, mTOR, p-mTOR, E-cadherin, Vimentin, and N-cadherin after adding Ki8751 to HCT116, and HCT8 cells.

    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

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.

    IC50 & Target

    VEGFR2

    0.9 nM (IC50)

    体外研究
    (In Vitro)

    Ki8751 inhibits VEGFR-2 phosphorylation at an IC50 value of 0.90 nM, and also inhibits the PDGFR family members such as PDGFRR and c-Kit at 67 nM and 40 nM, respectively. However, Ki8751 does not have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR and others even at 10000 nM. Ki8751 suppresses the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) on a nanomolar level[1].

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

    Ki8751 相关抗体:
    体内研究
    (In Vivo)

    Ki8751 shows significant antitumor activity against five human tumor xenografts such as GL07 (glioma), St-4 (stomach carcinoma), LC6 (lung carcinoma), DLD-1 (colon carcinoma) and A375 (melanoma) in nude mice and also shows complete tumor growth inhibition with the LC-6 xenograft in nude rats following oral administration once a day for 14 days at 5 mg/kg without any body weight loss[1].

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

    469.41

    Formula

    C24H18F3N3O4
    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
    细胞实验： 

    DMSO 中的溶解度 : 33.33 mg/mL (71.00 mM; 超声助溶 (<60°C); 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 2.1303 mL 10.6517 mL 21.3033 mL
    5 mM 0.4261 mL 2.1303 mL 4.2607 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

    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: 2.5 mg/mL (5.33 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      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 (5.33 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      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。
    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: 98.15%

    COA (291 KB) LCMS (96 KB)

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

    VEGFR-2 kinase assay is described below; GST-fusion proteins of KDR (Flk-1: cytoplasmic domain) are produced in the baculo-virus expression system. GST-KDR is premixed with a serial dilution of Ki8751 in the kinase buffer. The kinase reaction is initiated by the addition of 2 µM ATP in a solution of MnCl2. After 20 min incubation at room temperature, the reaction is stopped with an addition of EDTA. Phosphorylation levels of GST-KDR are detected by immunoblotting with anti-phosphotyrosine monoclonal antibodies (PY20) and detected by ECL fluorography[1].

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

    HUVECs are placed at a density of 4000 cells/200 µL/well on collagene type I precoated 96-well plates in M199 medium with 5% fetal bovine serum (FBS). After 24 h, the cells are incubated for 1 h in the presence or absence of Ki8751; then the cells are stimulated by rhVEGF (20 ng/mL). The cultures are incubated at 37 °C for 72 h, then pulsed with 1 µCi/well [3H]thymidine and reincubated for 14 h. Cells are assayed for the incorporation of tritium using a beta counter[1].

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

    Mice: The effects of Ki8751 on tumor growth is tested against various tumors, human stomach carcinoma (St-4), human lung carcinoma (LC-6), human colon carcinoma (DLD-1) and human melanoma (A375), using human tumor xenografts in nude mice. Ki8751 is administered orally to mice in the experimental groups once a day for 9 consecutive days at 5 mg/kg, and the vehicle is administered to control animals. Tumor volumes are monitored twice weekly[1].

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

    Ki8751 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 2.1303 mL 10.6517 mL 21.3033 mL 53.2583 mL
    5 mM 0.4261 mL 2.1303 mL 4.2607 mL 10.6517 mL
    10 mM 0.2130 mL 1.0652 mL 2.1303 mL 5.3258 mL
    15 mM 0.1420 mL 0.7101 mL 1.4202 mL 3.5506 mL
    20 mM 0.1065 mL 0.5326 mL 1.0652 mL 2.6629 mL
    25 mM 0.0852 mL 0.4261 mL 0.8521 mL 2.1303 mL
    30 mM 0.0710 mL 0.3551 mL 0.7101 mL 1.7753 mL
    40 mM 0.0533 mL 0.2663 mL 0.5326 mL 1.3315 mL
    50 mM 0.0426 mL 0.2130 mL 0.4261 mL 1.0652 mL
    60 mM 0.0355 mL 0.1775 mL 0.3551 mL 0.8876 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:

    Ki8751228559-41-9Ki 8751Ki-8751VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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