1067997-59-4Relevant articles and documents
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors
Kunz, Roxanne K.,Rumfelt, Shannon,Chen, Ning,Zhang, Dawei,Tasker, Andrew S.,Buerli, Roland,Hungate, Randall,Yu, Violeta,Nguyen, Yen,Whittington, Douglas A.,Meagher, Kristin L.,Plant, Matthew,Tudor, Yanyan,Schrag, Michael,Xu, Yang,Ng, Gordon Y.,Hu, Essa
, p. 5115 - 5117 (2008)
Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors has been shown clinically to successfully treat gastrointestinal stromal tumors and mastocytosis. Targeted therapy of c-Kit activity may provide therapeutic advantages against off-target effects for non-oncology applications. A new structural class of c-Kit inhibitors is described, including in vitro c-Kit potency, kinase selectivity, and the observed binding mode.
