GB1107

GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a K d of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model In Vitro Treatment with GB1107 (0-1 μM) increases tumor M1 macrophage polarization and CD8+ T cell infiltration in LLC cells by flow cytometric analysis. GB1107 potentiates the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GB1107 (10 mg/kg, p.o., once daily from day 18-30 post implantation) treatment results in significantly reduced tumor growth and final tumor weights . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CD-1 nude female mice received 3x10 6 human lung adenocarcinoma cells (A549) . Dosage: 10 mg/kg Administration: Oral once daily from day 18-30 post implantation. Result: Resulted in significantly reduced tumor growth and final tumor weights. IC50& Target:Kd: 37 nM (human Gal-3)

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