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Description: UNC-2025 HCl (known also as UNC2025), the Hydrochloride salt of UNC-2025, is an orally bioavailable and selective MER/FLT3 dual inhibitor with potential antineoplastic activity. It inhibits MER/FLT3 kinases with IC50s of 0.74 nM and 0.8 nM, respectively. UNC 2025 displayed about 20-fold selectivity for inhibiting MER/FLT3 over Axl and Tyro3. UNC-2025 is also capable of inhibiting Mer phosphorylation in vivo and shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy.
References: J Med Chem. 2014 Aug 28; 57(16):7031-41; Mol Cancer Ther. 2015 Sep; 14(9):2014-22.
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