HER2


Receptor tyrosine-protein kinase erbB-2, also known as CD340 (cluster of differentiation 340), proto-oncogene Neu, Erbb2 (rodent), or ERBB2 (human). It is a protein that in humans is encoded by the ERBB2 gene, and it is also frequently called HER2 (from human epidermal growth factor receptor 2) or HER2/neu.
HER2 is a member of the human epidermal growth factor receptor (HER/EGFR/ERBB) family. Amplification or over-expression of this oncogene has been shown to play an important role in the development and progression of certain aggressive types of breast cancer. In recent years the protein has become an important biomarker and target of therapy for approximately 30% of breast cancer patients.
  • Afatinib EY1739

    Afatinib (BIBW2992)是一种不可逆EGFR/HER2抑制剂,对EGFR(wt), EGFR(L858R), EGFR(L858R/T790M)和HER2均有抑制作用,IC50分别为0.5 nM,0.4 nM,10 nM和14 nM;用于Gefitinib抗性的突变型EGFR (L858R-T790M )时,活性增强100倍。

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  • Neratinib EY1582

    Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂,IC50分别为59 nM和92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf和c-Met没有显著的抑制作用。

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  • Mubritinib EY1477

    Mubritinib(TAK-165)是HER2高效选择性抑制剂,IC50值为6nM,对EGFR、PDGFR、FGFR等激酶抑制剂基本无。

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  • CP-724714 EY0707

    CP-724714是一种有效的,选择性的HER2/ErbB2抑制剂,IC50为10 nM,比作用于EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met等选择性高640多倍。

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  • Lapatinib EY0007

    Lapatinib (GW572016) is a small-molecule dual inhibitor of EGFR and ErbB2 receptor kinase activities. Lapatinib可形成Lapatinib的二甲苯磺酸盐,是一种有效的EGFR和ErbB2抑制剂,IC50分别为10.2和9.8 nM。

    More
  • Afatinib EY1739

    Afatinib (BIBW2992)是一种不可逆EGFR/HER2抑制剂,对EGFR(wt), EGFR(L858R), EGFR(L858R/T790M)和HER2均有抑制作用,IC50分别为0.5 nM,0.4 nM,10 nM和14 nM;用于Gefitinib抗性的突变型EGFR (L858R-T790M )时,活性增强100倍。

    More
  • Neratinib EY1582

    Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂,IC50分别为59 nM和92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf和c-Met没有显著的抑制作用。

    More
  • Mubritinib EY1477

    Mubritinib(TAK-165)是HER2高效选择性抑制剂,IC50值为6nM,对EGFR、PDGFR、FGFR等激酶抑制剂基本无。

    More
  • CP-724714 EY0707

    CP-724714是一种有效的,选择性的HER2/ErbB2抑制剂,IC50为10 nM,比作用于EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met等选择性高640多倍。

    More
  • Lapatinib EY0007

    Lapatinib (GW572016) is a small-molecule dual inhibitor of EGFR and ErbB2 receptor kinase activities. Lapatinib可形成Lapatinib的二甲苯磺酸盐,是一种有效的EGFR和ErbB2抑制剂,IC50分别为10.2和9.8 nM。

    More
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