GB1107

• CAT Number: I019458
• CAS Number: 1978336-61-6
• Molecular Formula: C20H16Cl2F3N3O4S
• Molecular Weight: 522.32
• Purity: ≥95%
• Synonyms: (2R,3R,4S,5R,6R)-2-(3,4-dichlorophenyl)sulfanyl-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-3,5-diol
• InChI: InChI=1S/C20H16Cl2F3N3O4S/c21-10-2-1-9(5-11(10)22)33-20-19(31)17(18(30)15(7-29)32-20)28-6-14(26-27-28)8-3-12(23)16(25)13(24)4-8/h1-6,15,17-20,29-31H,7H2/t15-,17+,18+,19-,20-/m1/s1
• InChIKey: CSGJIUAIYDKFPC-DABHTEOTSA-N
• SMILES: C1=CC(=C(C=C1SC2C(C(C(C(O2)CO)O)N3C=C(N=N3)C4=CC(=C(C(=C4)F)F)F)O)Cl)Cl

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].
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].
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].

Reference

[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.
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