Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
第一作者:
Ashvinikumar V,Gavai
第一单位:
Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, New Jersey 08543, USA. ashvinikumar.gavai@bms.com
作者:
主题词
投药, 口服(Administration, Oral);动物(Animals);抗肿瘤药(Antineoplastic Agents);生物利用度(Biological Availability);氨甲酸酯类(Carbamates);细胞系, 肿瘤(Cell Line, Tumor);狗(Dogs);药物筛选试验, 抗肿瘤(Drug Screening Assays, Antitumor);人类(Humans);成束猴(Macaca fascicularis);小鼠(Mice);肿瘤移植(Neoplasm Transplantation);立体异构现象(Stereoisomerism);构效关系(Structure-Activity Relationship);移植, 异种(Transplantation, Heterologous);三嗪类(Triazines)
DOI
10.1021/jm9010065
PMID
19821562
发布时间
2018-12-01
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