Description: NVP-BSK805 is a novel, potent and selective ATP-competitive JAK2 inhibitor with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. It displays more than 20-fold selectivity towards JAK2 in vitro. NVP-BSK805 also has excellent selectivity in broader kinase profiling. In vivo, NVP-BSK805 exhibited good oral bioavailability and a long half-life. The inhibitor was efficacious in suppressing leukemic cell spreading and splenomegaly in a Ba/F3 JAK2(V617F) cell-driven mouse mechanistic model. Furthermore, NVP-BSK805 potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.

References: Mol Cancer Ther. 2010 Jul;9(7):1945-55; BMC Cancer. 2011 Jan 19;11:24.

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