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Discovery of WS-157 as a highly potent,selective and orally active EGFR inhibitor 被引量:2
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作者 Pengxing He shenghui niu +7 位作者 Shuai Wang Xiaojing Shi Siqi Feng Linna Du Xuyang Zhang Zhilu Ma Bin Yu Hongmin Liu 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2019年第6期1193-1203,共11页
EGFR tyrosine kinase inhibitor(EGFR-TKI)has been used successfully in clinic for the treatment of solid tumors.In the present study,we reported the discovery of WS-157 from our inhouse diverse compound library,which w... EGFR tyrosine kinase inhibitor(EGFR-TKI)has been used successfully in clinic for the treatment of solid tumors.In the present study,we reported the discovery of WS-157 from our inhouse diverse compound library,which was validated to be a potent and selective EGFR-TKI.WS-157 showed excellent inhibitory activities against EGFR(IC50=0.81 nmol/L),EGFR[d746-750](IC50=1.2 nmol/L)and EGFR[L858R](IC50=1.1 nmol/L),but was less effective or even inactive against other nine kinases.WS-157 also displayed excellent antiproliferative activities against a panel of human cancer cell lines,and exhibited the ability to reduce colony formation and wound healing the same as gefitinib.We found that WS-157 upon oral administration showed better anti-tumor activity in A431 bearing xenograft mouse models compared to gefitinib.In addition,WS-157 showed better intestinal absorption than gefitinib and had favorable pharmacokinetic properties and microsomal metabolic stability in different species.These studies indicate that WS-157 has strong antitumor activity in vitro and in vivo,and could be used for the development of anti-lung cancer agent targeting EGFR. 展开更多
关键词 WS-157 TYROSINE KINASE EGFR INHIBITOR ANTITUMOR activity
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