| Description |
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model[1].
|
| Related Catalog |
|
| Target |
Kd: 37 nM (human Gal-3)[1].
|
| 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[1].
|
| 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[1]. Animal Model: CD-1 nude female mice received 3x106 human lung adenocarcinoma cells (A549)[1]. 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.
|
| References |
[1]. Vuong L, et al. An orally active galectin-3 antagonist inhibits lung adenocarcinoma growth and augments response to PD-L1 blockade. Cancer Res. 2019 Jan 23. pii: canres.2244.2018.
|
