1705602-02-3

GNE-4997 is a potent and selective ITK inhibitor (Ki = 0.09 nM).

GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity[1].

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[1] Burch JD, et al. Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo. J Med Chem. 2015 May 14;58(9):3806-16. DOI:10.1021/jm501998m