间变性淋巴瘤激酶
铈替尼
碱性抑制剂
化学
体内
药代动力学
药理学
克里唑蒂尼
体外
癌症研究
激酶
肺癌
医学
肿瘤科
生物化学
生物
生物技术
恶性胸腔积液
作者
Debasis Das,Jingbing Wang,Yong Li,Jingli Shi,Jian Hong
标识
DOI:10.1016/j.bmcl.2019.04.012
摘要
Anaplastic lymphoma kinase (ALK) is an attractive therapeutic target for the treatment of non-small cell lung cancer (NSCLC). Within our ALK drug discovery program, we identified novel deuterated 2,4-diarylamino pyrimidine compounds as potent ALK inhibitors. The compound 11 showed better in vitro activity and in vivo efficacy with good pharmacokinetic profile. In vivo efficacy of compound 11 was better than standard drug ceritinib in NCI-H2228 xenograft mice model.
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