For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019192 |
| CAS Number | 929300-19-6 |
| Synonyms | (5-aminopyridin-2-yl)-[9-[(2,2-dimethyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone |
| Molecular Formula | C26H34N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H34N4O2/c1-25(2)16-21-19(4-3-5-23(21)32-25)18-29-12-8-26(9-13-29)10-14-30(15-11-26)24(31)22-7-6-20(27)17-28-22/h3-7,17H,8-16,18,27H2,1-2H3 |
| InChIKey | WIGFMKMFRGRSDE-UHFFFAOYSA-N |
| SMILES | CC1(CC2=C(C=CC=C2O1)CN3CCC4(CC3)CCN(CC4)C(=O)C5=NC=C(C=C5)N)C |
| Reference | [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. |
