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rdf:type |
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lifeskim:mentions |
umls-concept:C0014898,
umls-concept:C0031727,
umls-concept:C0034802,
umls-concept:C0086418,
umls-concept:C0205531,
umls-concept:C0220825,
umls-concept:C0226896,
umls-concept:C0442027,
umls-concept:C0647750,
umls-concept:C1527415,
umls-concept:C1541473,
umls-concept:C1611588,
umls-concept:C1709630,
umls-concept:C1880355,
umls-concept:C1999216
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pubmed:issue |
21
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pubmed:dateCreated |
2009-11-5
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pubmed:abstractText |
Structure-activity relationships in a series of 4-[1H-indazol-5-ylamino]pyrrolo[2,1-f][1,2,4]triazine-6-carbamates identified dual human epidermal growth factor receptor (HER)1/HER2 kinase inhibitors with excellent biochemical potency and kinase selectivity. On the basis of its favorable pharmacokinetic profile and robust in vivo activity in HER1 and HER2 driven tumor models, 13 (BMS-599626) was selected as a clinical candidate for treatment of solid tumors.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Carbamates,
http://linkedlifedata.com/resource/pubmed/chemical/EGFR protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/HER2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Epidermal Growth Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, erbB-2,
http://linkedlifedata.com/resource/pubmed/chemical/Triazines
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:FairfaxDavid JDJ,
pubmed-author:FargnoliJosephJ,
pubmed-author:FinkBrian EBE,
pubmed-author:GavaiAshvinikumar VAV,
pubmed-author:GoyalBinduB,
pubmed-author:HanWen-ChingWC,
pubmed-author:HolstChristian LCL,
pubmed-author:KimSoong-HoonSH,
pubmed-author:LeavittKenneth JKJ,
pubmed-author:LeeFrancis YFY,
pubmed-author:MarathePunitP,
pubmed-author:MartinGregory SGS,
pubmed-author:MastalerzHaroldH,
pubmed-author:MathurArvindA,
pubmed-author:NorrisDerekD,
pubmed-author:OppenheimerSimoneS,
pubmed-author:PatelBharatB,
pubmed-author:RossiterLana MLM,
pubmed-author:SwaminathanShankarS,
pubmed-author:TokarskiJohn SJS,
pubmed-author:ViteGregory DGD,
pubmed-author:VyasDolatrai MDM,
pubmed-author:WongTai WTW,
pubmed-author:YuChiangC,
pubmed-author:ZhangHongjianH
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pubmed:issnType |
Electronic
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pubmed:day |
12
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6527-30
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pubmed:meshHeading |
pubmed-meshheading:19821562-Administration, Oral,
pubmed-meshheading:19821562-Animals,
pubmed-meshheading:19821562-Antineoplastic Agents,
pubmed-meshheading:19821562-Biological Availability,
pubmed-meshheading:19821562-Carbamates,
pubmed-meshheading:19821562-Cell Line, Tumor,
pubmed-meshheading:19821562-Dogs,
pubmed-meshheading:19821562-Drug Screening Assays, Antitumor,
pubmed-meshheading:19821562-Humans,
pubmed-meshheading:19821562-Macaca fascicularis,
pubmed-meshheading:19821562-Mice,
pubmed-meshheading:19821562-Neoplasm Transplantation,
pubmed-meshheading:19821562-Receptor, Epidermal Growth Factor,
pubmed-meshheading:19821562-Receptor, erbB-2,
pubmed-meshheading:19821562-Stereoisomerism,
pubmed-meshheading:19821562-Structure-Activity Relationship,
pubmed-meshheading:19821562-Transplantation, Heterologous,
pubmed-meshheading:19821562-Triazines
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pubmed:year |
2009
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pubmed:articleTitle |
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.
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pubmed:affiliation |
Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, New Jersey 08543, USA. ashvinikumar.gavai@bms.com
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pubmed:publicationType |
Journal Article
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