AZ084 是一种具有口服活性的选择性 CCR8 的变构拮抗剂，其Ki 值为 0.9 nM。AZ084 可通过下调 Treg 的分化来抑制免疫耐受性 PMN 的形成和肿瘤细胞在肺部的转移。AZ084 可用于哮喘和癌症的研究。
货号:ajcx39140
CAS:929300-19-6
分子式:C26H34N4O2
分子量：434.57
溶解度:DMSO : 250 mg/mL (575.28 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma[1]. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer[1][2].

AZ084 (5 μg/mL; single daily for 4 days) suppresses proportion of Tregs and reduces T cells that expresses CCR8 (co-cultured in vitro with LLC-exo MPF CM)[1].AZ084 (0-10 µM) inhibits AML, DC and T cells with IC50s of 1.3, 4.6 and 5.7 nM, respectively[2].

AZ084 (5 mg/kg; i.p.; every third day for 9 or 21 days) restrains the formation of the immunologically tolerant PMN and tumor cells metastasis in lung by downregulating Treg differentiation[1].AZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats[2].

[1]. 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.

Protocol:

CCR8 0.9nM(Ki)