2. Protein Tyrosine Kinase/RTK Apoptosis
  3. VEGFR Apoptosis
  4. Cabozantinib S-malate

Cabozantinib S-malate  (Synonyms: 卡博替尼苹果酸盐; XL184 S-malate; BMS-907351 S-malate)

目录号: HY-12044 纯度: 99.90%
COA 产品使用指南

摩尔计算器

Cabozantinib S-malate (XL184 S-malate) 是一种有效的多受体酪氨酸激酶抑制剂， 抑制VEGFR2，c-Met，Kit，Axl 和 Flt3 的 IC50 分别为0.035，1.3，4.6，7 和 11.3 nM。

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Cabozantinib S-malate Chemical Structure

Cabozantinib S-malate Chemical Structure

CAS No. : 1140909-48-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥503
In-stock
5 mg ￥360
In-stock
10 mg ￥570
In-stock
50 mg ￥1140
In-stock
100 mg ￥1680
In-stock
200 mg ￥2880
In-stock
500 mg   询价  
1 g   询价  

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Customer Review

Other Forms of Cabozantinib S-malate:

Cabozantinib S-malate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 41 篇科研文献

WB

    Cabozantinib S-malate 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 S-malate 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 S-malate 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 S-malate 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

    查看 VEGFR 亚型特异性产品:

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    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

    Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

    IC50 & Target[1]

    VEGFR2

    0.035 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    ≥ 50 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    BaF3 IC50
    0.01986 μM
    Compound: Cabozantinib L-malate
    Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay
    		[PMID: 27068889]
    EBC-1 IC50
    5.4 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    HUVEC IC50
    0.045 μM
    Compound: Cabozantinib L-malate
    Antiproliferative activity against recombinant human VEGF-stimulated HUVEC after 120 hrs by CCK8 assay
    Antiproliferative activity against recombinant human VEGF-stimulated HUVEC after 120 hrs by CCK8 assay
    		[PMID: 27068889]
    HUVEC IC50
    48.6 nM
    Compound: Cabozantinib L-Malate
    Cytotoxicity against HUVEC after 96 hrs by MTT assay
    Cytotoxicity against HUVEC after 96 hrs by MTT assay
    		[PMID: 30248654]
    NCI-H460 IC50
    45.5 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    SNU-5 IC50
    13.2 nM
    Compound: Cabozantinib L-Malate
    Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay
    Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay
    		[PMID: 30248654]
    体外研究
    (In Vitro)

    Cabozantinib (0.1-0.5 μM) 在所有 MPNST 细胞中抑制组成型和诱导型 MET 磷酸化及其产生的下游信号传导。Cabozantinib (> 0.1 μM) 引起显著的 MPNST 细胞生长抑制；需要更高的 Cabozantinib 剂量来抑制 NSC 生长。Cabozantinib 处理可阻断 HGF 诱导的 MPNST 运动和侵袭 (与在 NSC 上发现的类似作用)[2]。
    在细胞试验中，Cabozantinib 抑制 MET 和 VEGFR2 以及 KIT、FLT3 和 AXL 的磷酸化，IC50 值分别为 7.8、1.9、5.0、7.5 和 42 μM。Cabozantinib 还抑制小管形成，以响应来自 MDA-MB-231 (IC50=5.1 nM)、A431 (IC50=4.1 nM) 培养物的条件培养基，HT1080 (IC50=7.7 nM) 和 B16F10 (IC50=4.7 nM) 细胞[3]。

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

    Cabozantinib S-malate 相关抗体:
    体内研究
    (In Vivo)

    Cabozantinib (60 mg/kg, i.p.) 可减少动物肿瘤血管分布，连续 7 天，减少范围从 3 mg/kg 时的 67% 到 30 mg/kg 时的 83%。 与媒介物的相应值相比，从 10 周龄开始治疗 7 天的 RIP-Tag2 小鼠的肿瘤在 XL880 治疗后缩小了 40%，在 Cabozantinib 治疗后缩小了 35%[1]。
    Cabozantinib (30 mg/kg) 显着降低小鼠的微血管密度[2]。
    Cabozantinib（100 mg/kg，口服）可抑制肝细胞中 HGF 对 MET 磷酸化的体内刺激和 VEGF 刺激的 FLK1 磷酸化，并在给药后 8 小时内持续抑制这两个靶标。 Cabozantinib（100 mg/kg，口服）会破坏肿瘤血管系统并促进肿瘤和内皮细胞死亡。Cabozantinib（1-60 mg/kg，口服）可抑制体内肿瘤生长并促进肿瘤消退[3]。

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

    635.59

    Formula

    C32H30FN3O10
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    卡博替尼苹果酸盐；苹果酸卡博替尼
    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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (157.33 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 1.5733 mL 7.8667 mL 15.7334 mL
    5 mM 0.3147 mL 1.5733 mL 3.1467 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.90%

    COA (193 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [3]

    The inhibition profile of cabozantinib against a broad panel of 270 human kinases is determined using luciferase-coupled chemiluminescence, 33P-phosphoryl transfer, or AlphaScreen technology. Recombinant human full-length, glutathione S-transferase tag, or histidine tag fusion proteins are used, and half maximal inhibitory concentration (IC50) values are determined by measuring phosphorylation of peptide substrate poly (Glu, Tyr) at ATP concentrations at or below the Km for each respective kinase. The mechanism of kinase inhibition is evaluated using the AlphaScreen Assay by determining the IC50 values over a range of ATP concentrations.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [3]

    Cells are seeded in triplicate overnight in media containing 10% FBS. The next day, cells are treated with serial dilutions of cabozantinib for 48 hours, followed by analysis of proliferation using Cell Proliferation ELISA, BrdUrd.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    H441 cells (3×106) are implanted intradermally into the hind flank and when tumors reach approximately 150 mg, tumor weight is calculated using the formula: (tumor volume=length (mm) × width2 (mm2)]/2, mice are randomized (n=5 per group) and orally administered a single 100 mg/kg dose of cabozantinib or vehicle. Tumors are collected at the indicated time points. Pooled tumor lysates are subjected to immunoprecipitation with anti-MET (SC161) and Western blotting with anti-phosphotyrosine MET (pY1230/34/35). After blot stripping, total MET is quantitated as a loading control. In a separate experiment, naive mice (n=5 per group) are administered a single 100 mg/kg dose of cabozantinib or vehicle, followed by intravenous administration of HGF (10 μg per mouse) 10 minutes before liver collection. Analysis of MET phosphorylation in liver lysates is as described above. In a separate experiment, naive mice (n=5 per group) are administered a single 100 mg/kg dose of cabozantinib or vehicle, followed by intravenous administration of VEGF (10 μg per mouse) 30 minutes before lung collection. Pooled lung lysates are subjected to immunoprecipitation with FLK1 (SC6251) and Western blotting with anti-phosphotyrosine (4G10). After blot stripping, total FLK1 is quantitated as a loading control.

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

    Cabozantinib S-malate 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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 1.5733 mL 7.8667 mL 15.7334 mL 39.3335 mL
    5 mM 0.3147 mL 1.5733 mL 3.1467 mL 7.8667 mL
    10 mM 0.1573 mL 0.7867 mL 1.5733 mL 3.9334 mL
    15 mM 0.1049 mL 0.5244 mL 1.0489 mL 2.6222 mL
    20 mM 0.0787 mL 0.3933 mL 0.7867 mL 1.9667 mL
    25 mM 0.0629 mL 0.3147 mL 0.6293 mL 1.5733 mL
    30 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3111 mL
    40 mM 0.0393 mL 0.1967 mL 0.3933 mL 0.9833 mL
    50 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.7867 mL
    60 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6556 mL
    80 mM 0.0197 mL 0.0983 mL 0.1967 mL 0.4917 mL
    100 mM 0.0157 mL 0.0787 mL 0.1573 mL 0.3933 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:

    Cabozantinib1140909-48-3XL184BMS-907351卡博替尼苹果酸盐苹果酸卡博替尼XL 184XL-184BMS907351BMS 907351VEGFRApoptosisVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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