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  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: 雙馬來酸鹽阿法替尼; BIBW 2992MA2)

目錄號(hào): HY-10261A 純度: 99.88%
COA 產(chǎn)品使用指南

Afatinib (BIBW 2992) dimaleate 是一種口服有效且不可逆的 ErbB 家族 (EGFR 和 HER2) 雙特異性抑制劑，對(duì) EGFRwt, EGFRL858R, EGFRL858R/T790M 和 HER2 的 IC50 值分別為 0.5 nM、0.4 nM、10 nM 和 14 nM。Afatinib dimaleate 可用于食管鱗狀細(xì)胞癌 (ESCC)、非小細(xì)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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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥218
In-stock
5 mg ￥437
In-stock
10 mg ￥700
In-stock
25 mg ￥1050
In-stock
50 mg ￥1365
In-stock
100 mg ￥1780
In-stock
500 mg ￥3738
In-stock
1 g ￥5488
In-stock
5 g   詢價(jià)  
10 g   詢價(jià)  

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Customer Review

Other Forms of Afatinib dimaleate:

MCE 顧客使用本產(chǎn)品發(fā)表的 64 篇科研文獻(xiàn)

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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    查看 p38 MAPK 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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

     

    體外研究
    (In Vitro)

    Afatinib dimaleate (100 nM) 充分防止調(diào)蛋白刺激的 HER3 磷酸化[1]。
    Afatinib dimaleate (0-10000 nM) 有效抑制異位表達(dá) EGFR 的 NIH-3T3 細(xì)胞的貼壁非依賴性增殖突變體，并抑制 H1666、H3255 和 NCI 1975 細(xì)胞的細(xì)胞增殖[1]。
    Afatinib dimaleate (48-72 h) 在 HKESC-1、HKESC-2、SLMT-1 和 EC-1 細(xì)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 中誘導(dǎo) G0/G1 細(xì)胞周期停滯[2]。
    Afatinib dimaleate (0-1 μM，24-48 h) 有效誘導(dǎo) HKESC-2 和 EC-1 細(xì)胞凋亡[2]。

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

    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.
    體內(nèi)研究
    (In Vivo)

    Afatinib dimaleate (0 -20 mg/kg，口服，每日一次，持續(xù) 25 天) 顯示顯著的腫瘤消退和 EGFR、HER2、HER3 和 AKT 磷酸化下調(diào)[1]。
    Afatinib dimaleate (15 mg/kg，口服，5 天加停 2 天，持續(xù)兩周) 強(qiáng)烈抑制 HKESC-2 腫瘤的生長[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 號(hào)
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    阿法替尼雙馬來酸酯
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

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

    DMSO 中的溶解度 : ≥ 35 mg/mL (48.74 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： PBS

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

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.88%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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    產(chǎn)品名稱：
    Afatinib dimaleate
    目錄號(hào)：
    HY-10261A
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