1. Protein Tyrosine Kinase/RTK Apoptosis
  2. c-Met/HGFR Apoptosis
  3. Capmatinib

Capmatinib  (Synonyms: 卡马替尼; INC280; INCB28060)

目录号: HY-13404 纯度: 99.92%
COA 产品使用指南

Capmatinib (INC280; INCB28060) 是一种有效的、口服活性的、选择性的、ATP 竞争性的 c-Met 激酶抑制剂 (IC50=0.13 nM)。Capmatinib 可抑制 c-MET 的磷酸化,以及 c-MET 通路下游效应蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。Capmatinib 有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移,并有效诱导细胞凋亡。在肿瘤小鼠模型中表现出抗肿瘤活性。Capmatinib 主要由 CYP3A4 和醛氧化酶代谢。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Capmatinib Chemical Structure

Capmatinib Chemical Structure

CAS No. : 1029712-80-8

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     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 ¥869
In-stock
1 mg ¥320
In-stock
5 mg ¥790
In-stock
10 mg ¥950
In-stock
25 mg ¥1950
In-stock
50 mg ¥3100
In-stock
100 mg ¥4850
In-stock
200 mg 现货 询价
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

    Capmatinib purchased from MCE. Usage Cited in: Department Cancer Biology. Wayne State University. 2014 Jan.

    The c-Met Inhibitor INC280 Reveals HGF Activation of c-Met Leads to β4 Activation. (A) Dose-dependent assay to determine the concentration of INC280 required to prevent HGF-induced c-Met phosphorylation. Cells are pre-treated for two hours with INC280 at the indicated concentrations and then stimulated with 50 ng/mL HGF for 30 minutes. Phosphorylated (upper panel) and total c-Met (lower panel) are analyzed by Western blot. Densitometry represents the ratio of phosphorylated to total c-Met as a p
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].

    IC50 & Target

    IC50: 0.13 nM (c-MET)[1]

    体外研究
    (In Vitro)

    Capmatinib (INCB28060) 抑制 c-MET 磷酸化,IC50 值约为 1 nM,浓度约为 4 nM 时抑制 c-MET 超过 90%,这是可逆的,在去除化合物后的数小时内效果显著降低,48 小时后完全消失[1]
    Capmatinib (INCB28060) (0-10000 nM;72 小时) 抑制 SNU-5,S114、H441 和 U-87MG 的增殖[1]
    Capmatinib (INCB28060) (0.06-62.25 nM;2h) 有效抑制 c-MET 磷酸化以及 c-MET 通路下游效应子,例如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5[1]
    Capmatinib (INCB28060) (0.24-63 nM;过夜) 可防止 HGF 刺激的 H441 细胞迁移[1]
    Capmatinib (INCB28060) (0.5-50 nM;20 分钟) 可快速抑制 EGFR 和 HER-3 的磷酸化[1]
    Capmatinib (INCB28060) (0-333 nM;24 h) 诱导 SNU-5 细胞凋亡[1]

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

    Cell Viability Assay[1]

    Cell Line: SNU-5, S114, H441 and U-87MG
    Concentration: 0-10000 nM
    Incubation Time: 72 h
    Result: Inhibited the cell viability of SNU-5 and S114, as well as the colony formation of H441 and U-87MG, with IC50 values of 1.2 nM, 12.4 nM, ~0.5 nM and 2 nM, respectively.

    Cell Migration Assay [1]

    Cell Line: H441 (stimulated with 50 ng/mL recombinant human HGF for 24h)
    Concentration: 0.24, 1, 4, 16 and 63 nM
    Incubation Time: Over night
    Result: Prevented HGF-stimulated H441 cell migration, with IC50 of approximately 2 nM, and less cell migration at 16 nM.

    Western Blot Analysis[1]

    Cell Line: SNU-5
    Concentration: 0.06, 0.24, 0.98, 3.91, 15.63 and 62.25 nM
    Incubation Time: 2 h
    Result: Effectively inhibited phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.

    Western Blot Analysis[1]

    Cell Line: H1993 cells
    Concentration: 0.5, 5 and 50 nM
    Incubation Time: 20 min
    Result: Suppressed phosphorylation of both EGFR and HER-3 rapidly and as effectively as the compound inhibited c-MET phosphorylation in H1993 cells.

    Apoptosis Analysis[1]

    Cell Line: SNU-5 cells
    Concentration: 0.017, 0.15, 1.37, 12.33, 111 and 333 nM
    Incubation Time: 24 h
    Result: Effectively induced DNA fragmentation.
    体内研究
    (In Vivo)

    Capmatinib (INCB28060) (1-30 mg/kg;PO,每天两次,持续 2 周) 对肿瘤生长具有剂量依赖性抑制作用,并且在处理期间对所有剂量均表现出良好的耐受性,没有明显的毒性或体重的的损失证据在 U-87MG 肿瘤小鼠模型[1]
    Capmatinib (INCB28060) (0.03-10 mg/kg;PO,单剂量) 抑制 S114 肿瘤中的 c-MET 磷酸化小鼠模型[1]

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

    Animal Model: Female Balb/c nu/nu mice (inoculated subcutaneously with 5×106 U-87MG glioblastoma cells)[1]
    Dosage: 1, 3, 10 and 30 mg/kg
    Administration: PO, twice daily, for 2 weeks
    Result: Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.
    Animal Model: Female Balb/c nu/nu mice (inoculated subcutaneously with 4×106 S114 tumor cells)[1]
    Dosage: 0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
    Administration: PO, single dosage
    Result: Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.
    Clinical Trial
    分子量

    412.42

    Formula

    C23H17FN6O

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    卡马替尼;苯扎米特

    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 : 5 mg/mL (12.12 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)

    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 2.4247 mL 12.1236 mL 24.2471 mL
    5 mM 0.4849 mL 2.4247 mL 4.8494 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:

    以下溶解方案,请直接配制工作液。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-Na/saline water

      Solubility: 10 mg/mL (24.25 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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.92%

    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。-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 2.4247 mL 12.1236 mL 24.2471 mL 60.6178 mL
    5 mM 0.4849 mL 2.4247 mL 4.8494 mL 12.1236 mL
    10 mM 0.2425 mL 1.2124 mL 2.4247 mL 6.0618 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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Capmatinib
    目录号:
    HY-13404
    需求量: