2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Autophagy Apoptosis PI3K/Akt/mTOR
  3. EGFR Autophagy Apoptosis c-Met/HGFR Akt
  4. Afatinib oxalate

Afatinib oxalate  (Synonyms: BIBW 2992 oxalate)

目录号: HY-10261D
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摩尔计算器

Afatinib (BIBW 2992) oxalate 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 oxalate 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 oxalate Chemical Structure

Afatinib oxalate Chemical Structure

CAS No. : 1398312-64-5

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Afatinib oxalate 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 oxalate 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 oxalate 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 oxalate 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 oxalate 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) oxalate 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 oxalate 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

    EGFRL858R

    0.4 nM (IC50)

    EGFRWT

    0.5 nM (IC50)

    EGFRL858R/T790M

    10 nM (IC50)

    HER2

    14 nM (IC50)

    HER3

     

    体外研究
    (In Vitro)

    Afatinib oxalate (100 nM) sufficiently prevents heregulin-stimulated HER3 phosphorylation[1].
    Afatinib oxalate (0-10000 nM) effectively inhibits anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants, and inhibits cell proliferation of H1666, H3255, and NCI 1975 cells[1].
    Afatinib oxalate (48-72 h)shows growth inhibition in HKESC-1, HKESC-2, SLMT-1 and EC-1 cells[2].
    Afatinib oxalate (0-1 μM, 24-48 h) inhibits AKT and MAPK pathways, and inhibits EGFR and AKT phosphorylation in ESCC cell lines[2].
    Afatinib oxalate (0-1 μM, 16-48 h) induces G0/G1 cell cycle arrest in HKESC-2 and EC-1[2].
    Afatinib oxalate (0-1 μM, 24-48 h) effectively induces apoptotic cell death in HKESC-2 and EC-1[2].

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

    Afatinib oxalate 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 oxalate (0-20 mg/kg, Orally, daily for 25 days) shows dramatic tumor regression and downregulation of EGFR, HER2, HER3 and AKT phosphorylation[1].
    Afatinib oxalate (15 mg/kg, Orally, in a schedule of 5 days on plus 2 days off, for two weeks) strongly inhibits the growth of HKESC-2 tumor[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

    575.97

    Formula

    C26H27ClFN5O7
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Afatinib oxalate 相关分类

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    Keywords:

    Afatinib1398312-64-5BIBW 2992BIBW2992BIBW-2992EGFRAutophagyApoptosisc-Met/HGFRAktEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BNSCLCH1666H3255NCI-H1975NIH-3T3 cellsA431ESCCHER2AKTHKESC-1HKESC-2SLMT-1EC-1anticancerorally activelung cancerInhibitorinhibitorinhibit

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