Article
Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.
Blood - 15 Jun 2008
Hexner Elizabeth O, Serdikoff Cynthia, Jan Mahfuza, Swider Cezary R, Robinson Candy, Yang Shi, Angeles Thelma, Emerson Stephen G, Carroll Martin, Ruggeri Bruce, Dobrzanski Pawel
Abstract excerpt
Recent studies have demonstrated that patients with myeloproliferative disorders (MPDs) frequently have acquired activating mutations in the JAK2 tyrosine kinase. A multikinase screen determined that lestaurtinib (formerly known as CEP-701) inhibits wild type JAK2 kinase activity with a concentration that inhibits response by 50% (IC(50)) of 1 nM in vitro. We hypothesized that lestaurtinib would inhibit mutant...
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