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编 号:F245367
分子式:C20H16Cl2F3N3O4S
分子量:522.32
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
GB1107 (10 mg/kg,口服,植入后第 18-30 天每天一次) 处理可显著降低肿瘤生长和最终肿瘤重量。Animal Model:CD-1 nude female mice received 3x106 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.

体外研究:
通过流式细胞术分析,用 GB1107 (0-1 μM) 处理可增加 LLC 细胞中的肿瘤 M1 巨噬细胞极化和 CD8+ T 细胞浸润。GB1107 增强 PD-L1 免疫检查点抑制剂的作用,增加细胞毒性 (IFN-γ、颗粒酶 B、穿孔素-1、Fas 配体) 和凋亡 (裂解的 caspase-3) 效应分子的表达。
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