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.
体外研究
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.
体内研究
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.
Animal Model:
CD-1 nude female mice received 3x10 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.
分子式
C20H16Cl2F3N3O4S
分子量
522.32
CAS号
1978336-61-6
运输条件
Room temperature in continental US; may vary elsewhere.