Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.

Li, Zhihong; Wang, Xianghong; Eksterowicz, John; Gribble, Michael W; Alba, Grace Q; Ayres, Merrill; Carlson, Timothy J; Chen, Ada; Chen, Xiaoqi; Cho, Robert; Connors, Richard V; DeGraffenreid, Michael; Deignan, Jeffrey T; Duquette, Jason; Fan, Pingchen; Fisher, Benjamin; Fu, Jiasheng; Huard, Justin N; Kaizerman, Jacob; Keegan, Kathleen S; Li, Cong; Li, Kexue; Li, Yunxiao; Liang, Lingming; Liu, Wen; Lively, Sarah E; Lo, Mei-Chu; Ma, Ji; McMinn, Dustin L; Mihalic, Jeffrey T; Modi, Kriti; Ngo, Rachel; Pattabiraman, Kanaka; Piper, Derek E; Queva, Christophe; Ragains, Mark L; Suchomel, Julia; Thibault, Steve; Walker, Nigel; Wang, Xiaodong; Wang, Zhulun; Wanska, Malgorzata; Wehn, Paul M; Weidner, Margaret F; Zhang, Alex J; Zhao, Xiaoning; Kamb, Alexander; Wickramasinghe, Dineli; Dai, Kang; McGee, Lawrence R

Li, Zhihong; Wang, Xianghong; Eksterowicz, John; Gribble, Michael W; Alba, Grace Q; Ayres, Merrill; Carlson, Timothy J; Chen, Ada; Chen, Xiaoqi; Cho, Robert; Connors, Richard V; DeGraffenreid, Michael; Deignan, Jeffrey T; Duquette, Jason; Fan, Pingchen; Fisher, Benjamin; Fu, Jiasheng; Huard, Justin N; Kaizerman, Jacob; Keegan, Kathleen S; Li, Cong; Li, Kexue; Li, Yunxiao; Liang, Lingming; Liu, Wen; Lively, Sarah E; Lo, Mei-Chu; Ma, Ji; McMinn, Dustin L; Mihalic, Jeffrey T; Modi, Kriti; Ngo, Rachel; Pattabiraman, Kanaka; Piper, Derek E; Queva, Christophe; Ragains, Mark L; Suchomel, Julia; Thibault, Steve; Walker, Nigel; Wang, Xiaodong; Wang, Zhulun; Wanska, Malgorzata; Wehn, Paul M; Weidner, Margaret F; Zhang, Alex J; Zhao, Xiaoning; Kamb, Alexander; Wickramasinghe, Dineli; Dai, Kang; McGee, Lawrence R.

Affiliation

Li Z; Departments of Therapeutic Discovery, Oncology Research, §Pharmaceutics, and â¥Pharmacokinetics and Drug Metabolism, Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.

J Med Chem ; 57(8): 3430-49, 2014 Apr 24.

Article in En | MEDLINE | ID: mdl-24641103

Subject(s)

Cyclin-Dependent Kinase 4/antagonists & inhibitors; Heterocyclic Compounds, 3-Ring/chemical synthesis; Naphthyridines/chemical synthesis; Protein Kinase Inhibitors/chemical synthesis; fms-Like Tyrosine Kinase 3/antagonists & inhibitors; Animals; Cyclin-Dependent Kinase 6/antagonists & inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Dogs; Drug Discovery; Heterocyclic Compounds, 3-Ring/pharmacology; Humans; Macaca fascicularis; Naphthyridines/pharmacology; Protein Kinase Inhibitors/pharmacokinetics; Protein Kinase Inhibitors/pharmacology; Rats; Structure-Activity Relationship; U937 Cells; fms-Like Tyrosine Kinase 3/genetics

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protein Kinase Inhibitors / Cyclin-Dependent Kinase 4 / Fms-Like Tyrosine Kinase 3 / Heterocyclic Compounds, 3-Ring / Naphthyridines Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2014 Document type: Article Affiliation country: United States Country of publication: United States

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