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Oncology

A novel inhibitor of kinase insert domain-containing receptor fights tumors

Published in Cancer Weekly, March 16th, 2004

A novel inhibitor of kinase insert domain-containing receptor fights tumors.

According to recent research from the United States, "a strategy for antagonizing vascular endothelial growth factor (VEGF)-induced angiogenesis is to inhibit the kinase activity of its receptor, kinase insert domain-containing receptor (KDR), the first committed and perhaps the last unique step in the VEGF signaling cascade."

"We synthesized a novel ATP-competitive KDR tyrosine kinase inhibitor that potently suppresses human and mouse KDR activity in enzyme (IC50 = 7.8 - 19.5 nM) and cell-based assays (IC50 = 8 nM). The compound was bioavailable in...

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