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LDN-211904 is an inhibitor of erythropoietin-producing hepatocellular carcinoma (Eph) receptors. In particular, it inhibits EphB3 (IC50 = 79 nM), a tyrosine kinase receptor (RTK) subtype expressed during embryonic development and following central nervous system damage and some cancer cell growth.1 At 5 µM, this compound was profiled for inhibitory activity against a panel of 288 kinases and found to inhibit most of the EphA and EphB receptor kinase subtypes except for EphA6 and EphA7, and is non-inhibitory towards the non-RTKs screened except for p38α, p38β, and Qik.1
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1. Structure-