2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Autophagy Apoptosis PI3K/Akt/mTOR MAPK/ERK Pathway
  3. EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK
  4. Afatinib dimaleate

Afatinib dimaleate  (Synonyms: 双马来酸盐阿法替尼; BIBW 2992MA2)

目录号: HY-10261A 纯度: 99.88%
COA 产品使用指南

摩尔计算器

Afatinib (BIBW 2992) dimaleate 是一种口服有效且不可逆的 ErbB 家族 (EGFR 和 HER2) 双特异性抑制剂，对 EGFRwt, EGFRL858R, EGFRL858R/T790M 和 HER2 的 IC50 值分别为 0.5 nM、0.4 nM、10 nM 和 14 nM。Afatinib dimaleate 可用于食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌的研究。

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Afatinib dimaleate Chemical Structure

Afatinib dimaleate Chemical Structure

CAS No. : 850140-73-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770
In-stock
1 mg ￥218
In-stock
5 mg ￥437
In-stock
10 mg ￥700
In-stock
50 mg ￥1900
In-stock
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200 mg   询价  

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Customer Review

Other Forms of Afatinib dimaleate:

Afatinib dimaleate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 53 篇科研文献

WB

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

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

    Afatinib dimaleate purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613.  [Abstract]

    Immunoblot analysis of U-CH1, MUG-Chor1 and Chor-IN-1 cells treated with Afatinib for 2 h or 48 h. Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s for each cell line are reported.

    Afatinib dimaleate purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613.  [Abstract]

    Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s of the different inhibitors are reported.

    Afatinib dimaleate purchased from MCE. Usage Cited in: Oncotarget. 2014 Dec 15;5(23):11971-85.  [Abstract]

    H460/MX20 cells are treated with varying concentrations (0–2.0 μM) of Afatinib for 48 h, or with 1.0 μM Afatinib for 24 h, 48 h and 72 h, respectively. ABCG2 protein levels are analyzed by Western blot. GAPDH is used as a loading control.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1][2][3][4].

    IC50 & Target[1]

    EGFRL858R

    0.4 nM (IC50)

    EGFR

    0.5 nM (IC50)

    EGFRL858R/T790M

    10 nM (IC50)

    HER2

    14 nM (IC50)

    HER3

     

    体外研究
    (In Vitro)

    Afatinib dimaleate (100 nM) 充分防止调蛋白刺激的 HER3 磷酸化[1]。
    Afatinib dimaleate (0-10000 nM) 有效抑制异位表达 EGFR 的 NIH-3T3 细胞的贴壁非依赖性增殖突变体，并抑制 H1666、H3255 和 NCI 1975 细胞的细胞增殖[1]。
    Afatinib dimaleate (48-72 h) 在 HKESC-1、HKESC-2、SLMT-1 和 EC-1 细胞[2]。
    Afatinib dimaleate (0-1 μM，24-48 h) 抑制 AKT 和 MAPK 通路，并抑制 ESCC 中的 EGFR 和 AKT 磷酸化cell lines[2]。
    Afatinib dimaleate (0-1 μM，16-48 h) 在 HKESC-2 和 EC-1 中诱导 G0/G1 细胞周期停滞[2]。
    Afatinib dimaleate (0-1 μM，24-48 h) 有效诱导 HKESC-2 和 EC-1 细胞凋亡[2]。

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

    Afatinib dimaleate 相关抗体:

    Cell Proliferation Assay[1]

    Cell Line: NIH-3T3 cells, H1666, H3255, and NCI 1975 cells
    Concentration: 0, 1, 10, 100, 1000, 10000 nM
    Incubation Time:
    Result: Effectively inhibited anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants. Showed inhibition of anchorage independent cell proliferation of various lung cancer cell lines (H1666, H3255, and NCI 1975 cells), with IC50 values of 60 nM, 0.7 nM and 99 nM, respectively.

    Cell Viability Assay[2]

    Cell Line: HKESC-1, HKESC-2, SLMT-1 and EC-1 cell lines
    Concentration:
    Incubation Time: 48 and 72 hours
    Result: Observed over 95% of growth inhibition. The respective IC50 concentrations at 48 hours (HKESC-1=0.078 μM, HKESC-2=0.115 μM, KYSE510=3.182 μM, SLMT-1=4.625 μM and EC-1=1.489 μM) and 72 hours (HKESC-1=0.002 μM, HKESC-2=0.002 μM, KYSE510=1.090 μM, SLMT-1=1.161 μM and EC-1=0.109 μM) were all in lower micro-molar range.

    Western Blot Analysis[2]

    Cell Line: HKESC-2 cells and EC-1 cells
    Concentration: 0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
    Incubation Time: 24 and 48 hours
    Result: Reduced the phosphorylation of EGFR and the endogenous expression level of HER2 receptors in ESCC cells. Suppressed AKT phosphorylation in a dose and time dependent manner. Significantly reduced the phosphorylation level of the downstream effectors of the AKT-mTOR axis especially in HKESC-2 cells. Inhibited the two major downstream pathways of the ErbB/HER axis, namely, AKT and MAPK pathways in ESCC cell lines.

    Cell Cycle Analysis[2]

    Cell Line: HKESC-2 cells and EC-1 cells
    Concentration: 0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
    Incubation Time: 16, 24, and 48 hours
    Result: Induced G0/G1 cell cycle arrest in both tested ESCC cell lines in a time and dose dependent manner. In HKESC-2 cells, the percentage of cells in G0/G1 phase was increased from 38.2% to 68.1% at 0.01 μM of afatinib and to 74.7% at 0.1 μM of afatinib, from 24 hours (82.4% G0/G1 arrest at 0.01 μM and 86.2% at 0.1 μM) to 48 hours (from 74.7% to 88.2% for 0.01 μM and 91.0% for 0.1 μM). In EC-1 cells, the percentage of cells arrested in the G0/G1 phase was increased from 59.1% to 66.6% and 72.2% at 24 and 48 hours respectively.

    Apoptosis Analysis[2]

    Cell Line: HKESC-2 cells and EC-1 cells
    Concentration: 0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
    Incubation Time: 24 and 48 hours
    Result: Effectively induced cell death by triggering apoptotic mechanisms in ESCC cell lines. Showed a stronger expression level of cleaved Poly (ADP-ribose) polymerase (PARP) in these cell lines.
    体内研究
    (In Vivo)

    Afatinib dimaleate (0 -20 mg/kg，口服，每日一次，持续 25 天) 显示显著的肿瘤消退和 EGFR、HER2、HER3 和 AKT 磷酸化下调[1]。
    Afatinib dimaleate (15 mg/kg，口服，5 天加停 2 天，持续两周) 强烈抑制 HKESC-2 肿瘤的生长[2]。

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

    Animal Model: Athymic NMRI-nu/nu female mice (21–31 g, five to six-week-old, transgenic murine lung cancer model and xenograft models)[1]
    Dosage: 15 mg/kg, 20 mg/kg
    Administration: Orally, daily for 25 days
    Result: Resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2% in a standard xenograft model of the epidermoid carcinoma cell line A431, and downregulation of EGFR and AKT phosphorylation. Induced regression of large tumors in this HER2-driven model, effectively controlled xenograft tumor formation by the NCIH1975 cell line, expressing EGFR L858R/T790M, with a T/C value of 12% for doses of 20 mg/kg. Induced more than 50% percent tumor reduction after a 4-week treatment period. Downregulated EGFR, HER2 and HER3 phosphorylation.
    Animal Model: Six weeks old female athymic nude mice (nu/nu) (16-20 g)[2]
    Dosage: 15 mg/kg
    Administration: Oral gavage in a schedule of 5 days on plus 2 days off, for two weeks
    Result: Strongly inhibited the growth of HKESC-2 tumor. Average tumor sizes of vehicle and treatment at end point are 348 ± 24 mm3 and 108 ± 36 mm3 respectively.
    Clinical Trial
    分子量

    718.08

    Formula

    C32H33ClFN5O11
    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    阿法替尼双马来酸酯
    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: 

    H2O 中的溶解度 : 50 mg/mL (69.63 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 35 mg/mL (48.74 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.3926 mL 6.9630 mL 13.9260 mL
    5 mM 0.2785 mL 1.3926 mL 2.7852 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。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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:

    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： PBS

      Solubility: 100 mg/mL (139.26 mM); 澄清溶液; 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

    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
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.88%

    COA (274 KB) LCMS (269 KB)

    产品使用指南 (1538 KB)
    参考文献

    Afatinib dimaleate 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 / H2O 1 mM 1.3926 mL 6.9630 mL 13.9260 mL 34.8151 mL
    5 mM 0.2785 mL 1.3926 mL 2.7852 mL 6.9630 mL
    10 mM 0.1393 mL 0.6963 mL 1.3926 mL 3.4815 mL
    15 mM 0.0928 mL 0.4642 mL 0.9284 mL 2.3210 mL
    20 mM 0.0696 mL 0.3482 mL 0.6963 mL 1.7408 mL
    25 mM 0.0557 mL 0.2785 mL 0.5570 mL 1.3926 mL
    30 mM 0.0464 mL 0.2321 mL 0.4642 mL 1.1605 mL
    40 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8704 mL
    H2O 50 mM 0.0279 mL 0.1393 mL 0.2785 mL 0.6963 mL
    60 mM 0.0232 mL 0.1161 mL 0.2321 mL 0.5803 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    Afatinib dimaleate850140-73-7BIBW 2992MA2阿法替尼双马来酸酯EGFRAutophagyApoptosisc-Met/HGFRAktp38 MAPKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BNSCLCH1666H3255NCI-H1975NIH-3T3 cellsA431ESCCHER2AKTHKESC-1HKESC-2SLMT-1EC-1anticancerorally activelung cancerInhibitorinhibitorinhibit

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