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达克替尼Dacomitinib是一种特异,不可逆的 ERBB 家族抑制剂,作用于 EGFR,ERBB2 和 ERBB4 的 IC50 分别为 6 nM,45.7 nM 和 73.7 nM。
中文别名:
(2E)-N-[4-[(3-氯-4-氟苯基)氨基]-7-甲氧基-6-喹唑啉基]-4-(1-哌啶基)-2-丁烯酰胺;
(达克替尼)游离;
PF299804,达克替尼;
达克米替尼
物化属性:
密度:1.344
PSA:82.87000
LOGP:5.81550
[1]. Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15;67(24):11924-32.
[2]. Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib. Mol Cancer Ther. 2012 Sep;11(9):1978-87.
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