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An orally bioavailable inhibitor of Mer and Flt3
UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).1 It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.1 UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.1 Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.1
1.Zhang, W., DeRychere, D., Hunter, D., et al.UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitorJ. Med. Chem.57(16)7031-7041(2014)
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