Article
Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research - 15 Aug 2012
Heinrich Michael C, Griffith Diana, McKinley Arin, Patterson Janice, Presnell Ajia, Ramachandran Abhijit, Debiec-Rychter Maria
Abstract excerpt
PURPOSE: To determine the potential of crenolanib, a potent inhibitor of PDGFRA, to treat malignancies driven by mutant PDGFRA. EXPERIMENTAL DESIGN: The biochemical activity of crenolanib was compared with imatinib using a panel of PDGFRA-mutant kinases expressed in several different cell line models, including primary gastrointestinal stromal tumors (GIST) cells. The antiproliferative activity of crenolanib was...
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