Resiquimod

方法: 为检测体内抗肿瘤活性，将 Resiquimod (2 mg/kg) 和 4D5 抗 HER2 抗体 (20 mg/kg) 腹腔注射给携带 CT26-HER2/neu 肿瘤的 Balb/cJ 小鼠，每周三次，持续 13 天。 结果: 13 天后，接受 Resiquimod 加抗体的小鼠肿瘤的生长速率显著降低。统计测试显示 4D5 和 Resiquimod 在降低肿瘤生长速率方面具有协同作用。[2]

方法: 金绒球头肾淋巴细胞 HKL 用 Resiquimod (0.175-32 μg/mL) 处理 12 h，使用 CCK8 assay 检测细胞活力。 结果: CCK8 测定结果显示，0.25-32 μg/mL Resiquimod 显著促进 HKL 增殖。[1] 方法: 外周血单核细胞 PBM 用 Resiquimod (0.01-100 μM) 处理 1-14 h，使用 Western Blot 方法检测靶点蛋白表达水平。 结果: 1 μM 的剂量足以改变 FcγR 的表达，更高的剂量不会导致更大的变化。FcγRIIa 的增加发生在晚期，而 γ 链的小幅增加出现在 3 h，但在 14 h 时更高。然而，FcγRIIb 蛋白在1 h 内减少，而 FcγRIIb 的转录物保持到 4 h。[2]

Ethanol:20 mg/mL (63.62 mM); DMSO:55 mg/mL (174.95 mM); H2O:< 1 mg/mL (insoluble or slightly soluble);

Resiquimod is dissolved in DMSO. For inhibition of lysosomal acidification, cells are incubated with 10?μM CQ for 1?h before Resiquimod (R848) treatment. After treatment, 20?μL of 5?mg/mL MTT is added to the plate. The plate is incubated at 22°C for 4?h, and 200?μL dimethyl sulfoxide is added to the plate to dissolve the reduced formazan. The plate is then read at 490?nm with a microplate reader. To determine the effect of Myd88 inhibition on R848-induced cell proliferation, the Myd88 inhibitor Pepinh-MYD and the control peptide Pepinh-Control are added to PBL at the concentration of 50?μM, and the plate is incubated at 22°C for 6?h. After incubation, the cells are treated with R848 and subjected to MTT assay as above. To determine the effect of NF-κB inactivation on R848-induced cell proliferation, BAY-11-7082, an irreversible inhibitor of IκB-α phosphorylation, is added to the cells at the concentration of 1?μM, and the plate is incubated at 22°C for 1?h. After incubation, the cells are treated with R848 and subjected to MTT assay as earlier. All experiments are performed three times.

Animal Models: Wild-type mice,TLR7-deficient mice,and MyD88-deficient mice. Formulation: saline. Dosages: 50 nmol. Administration: i.p.