Ontology highlight
ABSTRACT:
SUBMITTER: Zarrinkar PP
PROVIDER: S-EPMC2756206 | biostudies-literature | 2009 Oct
REPOSITORIES: biostudies-literature
Zarrinkar Patrick P PP Gunawardane Ruwanthi N RN Cramer Merryl D MD Gardner Michael F MF Brigham Daniel D Belli Barbara B Karaman Mazen W MW Pratz Keith W KW Pallares Gabriel G Chao Qi Q Sprankle Kelly G KG Patel Hitesh K HK Levis Mark M Armstrong Robert C RC James Joyce J Bhagwat Shripad S SS
Blood 20090804 14
Activating mutations in the receptor tyrosine kinase FLT3 are present in up to approximately 30% of acute myeloid leukemia (AML) patients, implicating FLT3 as a driver of the disease and therefore as a target for therapy. We report the characterization of AC220, a second-generation FLT3 inhibitor, and a comparison of AC220 with the first-generation FLT3 inhibitors CEP-701, MLN-518, PKC-412, sorafenib, and sunitinib. AC220 exhibits low nanomolar potency in biochemical and cellular assays and exce ...[more]