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Description: Gandotinib (formerly also known as LY2784544) is a novel, potent and selective JAK2 (Janus kinase) inhibitor with potential antitumor activity. It inhibits JAK2 with an IC50 of 3 nM, and shows 8- and 20-fold selectivity for JAK2 over JAK1 and JAK3. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Gandotinib effectively inhibited JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55?nM, respectively). In vivo, Gandotinib effectively inhibited STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP ascitic tumor cells and significantly reduced Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model.
References: Blood Cancer J. 2013 Apr 12; 3:e109.
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