Article
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412.
Cancer cell - 1 Jun 2002
Weisberg Ellen, Boulton Christina, Kelly Louise M, Manley Paul, Fabbro Doriano, Meyer Thomas, Gilliland D Gary, Griffin James D
Abstract excerpt
Constitutively activating FLT3 receptor mutations have been found in 35% of patients with acute myeloblastic leukemia (AML). Here we report the identification of a small molecule FLT3 tyrosine kinase inhibitor PKC412, which selectively induced G1 arrest and apoptosis of Ba/F3 cell lines expressing mutant FLT3 (IC(50) < 10 nM) by directly inhibiting the tyrosine kinase. Ba/F3-FLT3 cell lines made resistant to...
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