Antitumor activity of a novel EGFR tyrosine kinase inhibitor against human lung carcinoma in vitro and in vivo
文献类型：期刊论文
| 作者 | Xiong, Xishan2; Fu, Lili2; Wang, Li2; Cai, Houan2; Li, Lin2; Jiang, Hualiang1 ; Duan, Wenhu1; Mei, Changlin2
|
| 刊名 | INVESTIGATIONAL NEW DRUGS
 |
| 出版日期 | 2009-02 |
| 卷号 | 27期号:1页码:1-11 |
| 关键词 | EGFR SPC-A1 tyrosine kinase inhibitor quinazoline non-small cell lung cancer |
| ISSN号 | 0167-6997 |
| DOI | 10.1007/s10637-008-9132-5 |
| 文献子类 | Article |
| 英文摘要 | Treatment with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) has led to dramatic clinical improvement in selected patients with non-small cell lung cancer (NSCLC). However, intrinsic and acquired resistance to EGFR-TKI remains a common phenomenon. Novel EGFR-TKI, structurally different with erlotinib or gefitinib might be beneficial for patients with NSCLC. In this study, we examined the antitumor effect of a newly synthesized novel EGFR tyrosine kinase inhibitor (Zhao260054). In vitro studies in a panel of four different human lung cancer cell lines revealed that Zhao260054 inhibited cell proliferation with high potency and induced G(0)/G(1) arrest of cell cycle and apoptosis. Zhao260054 markedly reduced phosphorylation of EGFR and inhibited activation of ERK1/2 and AKT. Oral administration of Zhao260054 (200 mg/kg/day) to BALB/c nude mice bearing SPC-A1 xenografts significantly retarded tumor growth. In conclusion, Zhao260054 has potent antitumor activity on human lung cancer in vitro and in vivo. |
| WOS关键词 | GROWTH-FACTOR RECEPTOR ; GALLBLADDER ADENOCARCINOMA CELLS ; PREVIOUSLY TREATED PATIENTS ; CANCER CELLS ; GEFITINIB IRESSA ; PHASE-II ; ERLOTINIB ; ACTIVATION ; THERAPY ; FAILURE |
| 资助项目 | National 863 Plan in High Technology Progress[2002AA2Z3130] ; Shanghai Leading Academic Discipline Project[B902] |
| WOS研究方向 | Oncology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000261957000001 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279333]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物发现与设计中心 |
| 通讯作者 | Mei, Changlin |
| 作者单位 | 1.Chinese Acad Sci, Grad Sch, Shanghai Inst Mat Med, State Key Lab Drug Res,Drug Discovery & Design Ct, Shanghai 201203, Peoples R China 2.Second Mil Med Univ, Changzheng Hosp, Dept Internal Med, Nephrol Inst PLA, Shanghai 200003, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Xiong, Xishan,Fu, Lili,Wang, Li,et al. Antitumor activity of a novel EGFR tyrosine kinase inhibitor against human lung carcinoma in vitro and in vivo[J]. INVESTIGATIONAL NEW DRUGS,2009,27(1):1-11. |
| APA | Xiong, Xishan.,Fu, Lili.,Wang, Li.,Cai, Houan.,Li, Lin.,...&Mei, Changlin.(2009).Antitumor activity of a novel EGFR tyrosine kinase inhibitor against human lung carcinoma in vitro and in vivo.INVESTIGATIONAL NEW DRUGS,27(1),1-11. |
| MLA | Xiong, Xishan,et al."Antitumor activity of a novel EGFR tyrosine kinase inhibitor against human lung carcinoma in vitro and in vivo".INVESTIGATIONAL NEW DRUGS 27.1(2009):1-11. |
入库方式： OAI收割
来源：上海药物研究所
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