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Description: AZD1480 (AZD-1480) is a selective, orally bioavailable and ATP-competitive inhibitor of JAK2 (Janus-associated kinase) with potential antitumor activity. It inhibits JAK2 with an IC50 of 0.26 nM in a cell-free assay. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy, because JAK2 is upregulated/mutated in a variety of cancer cells, mediating STAT3 activation and playing a key role in tumor cell proliferation and survival.
References: Blood Cancer J. 2011 Dec; 1(12): e46; Mol Cancer Ther. 2011 Dec; 10(12):2384-93; Cancer Res. 2011 Nov 1; 71(21):6601-10.
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