生物活性 | |||
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描述 | AZ084 is a potent, selective, allosteric and orally active CCR8 antagonist with a Ki of 0.9 nM [1].AZ084 inhibits the formation of immunologically tolerant pre-metastatic niche (PMN) and metastasis of tumour cells in the lungs through down-regulation of Treg differentiation [1][2].Administered once daily for 4 days at a concentration of 5 μg/mL, AZ084 inhibits the proportion of Treg and reduces CCR8-expressing T cells (cultured ex vivo with LLC-exo MPF CM)[1][2].At concentrations of 0-10 μM, AZ084 inhibited AML, DC and T cells with IC50 values of 1.3 nM, 4.6 nM and 5.7 nM, respectively[2] . |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.51mL 2.30mL 1.15mL |
23.01mL 4.60mL 2.30mL |
参考文献 |
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