1. Protein Tyrosine Kinase/RTK Apoptosis
  2. VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis
  3. Cabozantinib

Cabozantinib  (Synonyms: 卡博替尼; XL184; BMS-907351)

目录号: HY-13016 纯度: 99.96%
COA 产品使用指南

Cabozantinib 是一种口服有效的 VEGFR2MET 抑制剂,IC50 分别为 0.035 和 1.3 nM。Cabozantinib 对 KITRETAXLTIE2FLT3 有较强的抑制作用 (IC50=4.6、5.2、7、14.3 和 11.3 nM)。Cabozantinib 显示出抗血管生成活性。Cabozantinib 可以破坏肿瘤血管,促进肿瘤和内皮细胞凋亡 (apoptosis)。

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Cabozantinib Chemical Structure

Cabozantinib Chemical Structure

CAS No. : 849217-68-1

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10 mM * 1 mL in DMSO ¥861
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5 mg ¥780
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10 mg ¥1100
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50 mg ¥2850
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100 mg ¥4000
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500 mg ¥7890
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 39 篇科研文献

WB

    Cabozantinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Nov;16(11):2387-2398.  [Abstract]

    Representative Western blots and densitometry show that cabozantinib reduces phosphorylation of Erk1/2 after 6 hours and reduces cyclin D1 and increases p27 protein levels after 24 hours of treatment (n=3-4).

    Cabozantinib purchased from MCE. Usage Cited in: PLoS One. 2017 Sep 25;12(9):e0185321.  [Abstract]

    Treatment with Cabozantinib results in complete inhibition of the c-MET phosphorylation stimulated by HGF at nanomolar concentrations.

    Cabozantinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.  [Abstract]

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

    Cabozantinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73.  [Abstract]

    Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1][2].

    IC50 & Target[1]

    VEGFR2

    0.035 nM (IC50)

    Flt-4

    6 nM (IC50)

    Flt-1

    12 nM (IC50)

    Met

    1.3 ± 1.2 nM (IC50)

    体外研究
    (In Vitro)

    Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively[1].
    Cabozantinib (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively[1].
    Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
    Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].

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

    Cell Proliferation Assay

    Cell Line: SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells[1]
    Concentration:
    Incubation Time: 48 hours
    Result: Inhibited tumor cell proliferation, with IC50 of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively.

    Cell Migration Assay

    Cell Line: B16F10 cells[1]
    Concentration: 0, 41, 123, and 370 nM
    Incubation Time: 24 hours
    Result: Potently inhibited HGF-induced migration (IC50 = 31 nM) of B16F10 cells.

    Cell Invasion Assay

    Cell Line: B16F10 cells[1]
    Concentration: 0, 1.5, 14, and 123 nM
    Incubation Time: 24 hours
    Result: Potently inhibited HGF-induced invasion (IC50 = 9 nM) of B16F10 cells.
    体内研究
    (In Vivo)

    Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].
    Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
    Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].

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

    Animal Model: Female mice bearing MBA-MB-231 tumor (5 per group)[1]
    Dosage: 0, 100 mg/kg
    Administration: Orally, once
    Result: Inhibited MET and VEGFR2 phosphorylation.
    Animal Model: Mice bearing MBA-MB-231 tumor[1]
    Dosage: 1, 3, 10, 30, 60 mg/kg
    Administration: Orally, once daily for 14 days
    Result: Inhibited tumor growth in a dose-dependent manner.
    Clinical Trial
    分子量

    501.51

    Formula

    C28H24FN3O5

    CAS 号
    性状

    固体

    颜色

    White to gray

    中文名称

    卡博替尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 25 mg/mL (49.85 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 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9940 mL 9.9699 mL 19.9398 mL
    5 mM 0.3988 mL 1.9940 mL 3.9880 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 (protect from 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。

    • 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: 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.98 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.15 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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。

    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: 0.5% CMC/saline water

      Solubility: 2.5 mg/mL (4.98 mM); 悬浊液; 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

    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 (protect from 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: 99.96%

    参考文献

    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 (protect from 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
    DMSO 1 mM 1.9940 mL 9.9699 mL 19.9398 mL 49.8495 mL
    5 mM 0.3988 mL 1.9940 mL 3.9880 mL 9.9699 mL
    10 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9849 mL
    15 mM 0.1329 mL 0.6647 mL 1.3293 mL 3.3233 mL
    20 mM 0.0997 mL 0.4985 mL 0.9970 mL 2.4925 mL
    25 mM 0.0798 mL 0.3988 mL 0.7976 mL 1.9940 mL
    30 mM 0.0665 mL 0.3323 mL 0.6647 mL 1.6616 mL
    40 mM 0.0498 mL 0.2492 mL 0.4985 mL 1.2462 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:
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    目录号:
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