产品说明书

AZ084

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Chemical Structure| 929300-19-6 同义名 : -
CAS号 : 929300-19-6
货号 : A1177059
分子式 : C26H34N4O2
纯度 : 99%
分子量 : 434.574
MDL号 : MFCD32062782
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(575.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[1]Wang M, et al. Tumor-derived exosomes drive pre-metastatic niche formation in lung via modulating CCL1+ fibroblast and CCR8+ Treg cell interactions. Cancer Immunol Immunother. 2022 Apr 15.

[2]Connolly S, et al. Orally bioavailable allosteric CCR8 antagonists inhibit dendritic cell, T cell and eosinophil migration. Biochem Pharmacol. 2012 Mar 15;83(6):778-87.