873792-88-2Relevant articles and documents
Nucleotides and nucleosides and methods for their use in DNA sequencing
-
, (2015/12/18)
The present invention relates generally to labeled and unlabled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.
EC144 is a potent inhibitor of the heat shock protein 90
Shi, Jiandong,Van De Water, Ryan,Hong, Kevin,Lamer, Ryan B.,Weichert, Kenneth W.,Sandoval, Cristina M.,Kasibhatla, Srinivas R.,Boehm, Marcus F.,Chao, Jianhua,Lundgren, Karen,Timple, Noelito,Lough, Rachel,Ibanez, Gerardo,Boykin, Christina,Burrows, Francis J.,Kehry, Marilyn R.,Yun, Theodore J.,Harning, Erin K.,Ambrose, Christine,Thompson, Jeffrey,Bixler, Sarah A.,Dunah, Anthone,Snodgrass-Belt, Pamela,Arndt, Joseph,Enyedy, Istvan J.,Li, Ping,Hong, Victor S.,McKenzie, Andres,Biamonte, Marco A.
, p. 7786 - 7795 (2012/11/07)
Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl) methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol (EC144), is a second generation inhibitor of heat shock protein 90 (Hsp90) and is substantially more potent in vitro and in vivo than the first generation inhibitor 14 (BIIB021) that completed phase II clinical trials. Alkyne 40 is more potent than 14 in an Hsp90α binding assay (IC50 = 1.1 vs 5.1 nM) as well as in its ability to degrade Her-2 in MCF-7 cells (EC 50 = 14 vs 38 nM). In a mouse model of gastric tumors (N87), 40 stops tumor growth at 5 mg/kg and causes partial tumor regressions at 10 mg/kg (po, qd× 5). Under the same conditions, 14 stops tumor growth only at 120 mg/kg, and does not induce partial regressions. Thus, alkyne 40 is approximately 20-fold more efficacious than 14 in mice.