CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo

CYT997 is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. CYT997 blocks the cell cycle at the G 2 -M boundary, and Western blot analysis indicates an increase in phosphorylated Bcl-2, along with increased expressi...

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Veröffentlicht in:	Molecular cancer therapeutics 2009-11, Vol.8 (11), p.3036-3045
Hauptverfasser:	Burns, Christopher J, Fantino, Emmanuelle, Phillips, Ian D, Su, Stephen, Harte, Michael F, Bukczynska, Patricia E, Frazzetto, Mark, Joffe, Max, Kruszelnicki, Irma, Wang, Bing, Wang, Yue, Wilson, Neil, Dilley, Rodney J, Wan, Soo S, Charman, Susan A, Shackleford, David M, Fida, Rosa, Malcontenti-Wilson, Cathy, Wilks, Andrew F
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological Availability Cancer Cell Cycle - drug effects Cell Growth Processes - drug effects Cell Line, Tumor Cell Survival - drug effects cytotoxic Drug Screening Assays, Antitumor Endothelial Cells - drug effects Endothelial Cells - metabolism Female Humans inhibitor Lung Neoplasms - drug therapy Lung Neoplasms - metabolism Lung Neoplasms - pathology Male Mammary Neoplasms, Experimental - drug therapy Mammary Neoplasms, Experimental - metabolism Mammary Neoplasms, Experimental - pathology Mice Mice, Inbred BALB C Mice, Nude microtubules Prostatic Neoplasms - drug therapy Prostatic Neoplasms - metabolism Prostatic Neoplasms - pathology Pyridines - pharmacokinetics Pyridines - pharmacology Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Rats Rats, Sprague-Dawley tubulin Tubulin Modulators - pharmacokinetics Tubulin Modulators - pharmacology Xenograft Model Antitumor Assays
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