2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Neratinib maleate

Neratinib maleate  (Synonyms: HKI-272 maleate)

目录号: HY-32721B 纯度: 99.83%
COA 产品使用指南

摩尔计算器

Neratinib (HKI-272) maleate 是一种具有口服活性的、不可逆的、高选择性的 HER2 和 EGFR 抑制剂，IC50 值分别为 59 nM 和 92 nM。

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

Neratinib maleate Chemical Structure

Neratinib maleate Chemical Structure

CAS No. : 915942-22-2

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
Free Sample (0.1 - 0.2 mg)   Apply now  
5 mg ￥350
In-stock
10 mg ￥600
In-stock
25 mg ￥950
In-stock
50 mg ￥1300
In-stock
100 mg ￥2300
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Neratinib maleate:

Neratinib maleate 相关抗体

Top Publications Citing Use of Products

    Neratinib maleate purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jun 20;10(446):eaao2565.  [Abstract]

    Immunoblots of 3 individual KM tumors from mice treated for 3 days with Neratinib or vehicle control.

    Neratinib maleate purchased from MCE. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176.  [Abstract]

    Influence of BIBW 2992 or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.

    查看 EGFR 亚型特异性产品:

    查看所有亚型
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively[1].

    IC50 & Target

    HER2

    59 nM (IC50)

    EGFR

    92 nM (IC50)

    体外研究
    (In Vitro)

    Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met[1].
    Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) [1].
    Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase[1].
    Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27[1].

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

    Neratinib maleate 相关抗体:

    Cell Proliferation Assay[1]

    Cell Line: 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620
    Concentration: 0.5 ng/mL–5 μg/mL
    Incubation Time: 2 days (6 days for BT474)
    Result: Inhibited cell proliferation with IC50 values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.

    Western Blot Analysis[1]

    Cell Line: BT474 or A431 cells
    Concentration: 0, 2, 10, 50, 100 and 200 nM
    Incubation Time: 3 h
    Result: Decreased ligand-independent receptor phosphorylation by 50% (IC50) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC50 = 3 nM).
    Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.

    Cell Cycle Analysis[1]

    Cell Line: BT474
    Concentration: 0–2 nM
    Incubation Time: 12–16 h
    Result: Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.
    体内研究
    (In Vivo)

    Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR[1].

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

    Animal Model: Female athymic (nude) mice, tumor xenograft[1]
    Dosage: 10, 20, 40, 60 or 80 mg/kg/day
    Administration: Gavage, 42 days
    Result: Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.
    Clinical Trial
    分子量

    673.11

    Formula

    C34H33ClN6O7
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    马来酸来那替尼
    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
    In Vitro: 

    DMSO 中的溶解度 : 250 mg/mL (371.41 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 1.4856 mL 7.4282 mL 14.8564 mL
    5 mM 0.2971 mL 1.4856 mL 2.9713 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
    参考文献

    Neratinib maleate 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 1.4856 mL 7.4282 mL 14.8564 mL 37.1410 mL
    5 mM 0.2971 mL 1.4856 mL 2.9713 mL 7.4282 mL
    10 mM 0.1486 mL 0.7428 mL 1.4856 mL 3.7141 mL
    15 mM 0.0990 mL 0.4952 mL 0.9904 mL 2.4761 mL
    20 mM 0.0743 mL 0.3714 mL 0.7428 mL 1.8571 mL
    25 mM 0.0594 mL 0.2971 mL 0.5943 mL 1.4856 mL
    30 mM 0.0495 mL 0.2476 mL 0.4952 mL 1.2380 mL
    40 mM 0.0371 mL 0.1857 mL 0.3714 mL 0.9285 mL
    50 mM 0.0297 mL 0.1486 mL 0.2971 mL 0.7428 mL
    60 mM 0.0248 mL 0.1238 mL 0.2476 mL 0.6190 mL
    80 mM 0.0186 mL 0.0929 mL 0.1857 mL 0.4643 mL
    100 mM 0.0149 mL 0.0743 mL 0.1486 mL 0.3714 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:

    Neratinib915942-22-2HKI-272马来酸来那替尼HKI272HKI 272EGFREpidermal growth factor receptorErbB-1HER1breast cancersolid tumorsnon–small-cell lung cancerBT474A431gastric cancerInhibitorinhibitorinhibit

    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：
    Neratinib maleate
    目录号：
    HY-32721B
    需求量：

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * Lot #：

    * 客户姓名：

    		 

    * Email：

       电话：

    		 

    * 部门：

    * 公司或机构名称：

    		 

       留言给我们：

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.

    嗨！很高兴为您提供帮助！

    尊敬的 MCE 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z