Description
ARB-272572 is a novel potent PD-L1 inhibitor, inducing PD-L1 dimerization and internalization.
Uses
ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC50 value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections[1][2].
in vivo
ARB-272572 (10 mg/kg; oral; once daily; seven days) inhibits tumor growth in humanized colon cancer mice[1].
| Animal Model: | Humanized mouse model of colon cancer [1] |
| Dosage: | 10 mg/kg; daily; 7 days |
| Administration: | Oral |
| Result: | Reduced tumor volume, tumor regression, and the number of CD3+ T cells in peripheral blood increased, especially CD4+ T cells significantly increased, while the proportion of regulatory T cells decreased significantly. |
References
[1] Park JJ, et al. Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1. Nat Commun. 2021 Feb 22;12(1):1222. DOI:
10.1038/s41467-021-21410-1[2] Zhijie Wang, et al. Reducing PD-L1 Expression by Degraders and Downregulators as a Novel Strategy to Target the PD-1/PD-L1 Pathway. J Med Chem. 2024 Apr 25;67(8):6027-6043. DOI:
10.1021/acs.jmedchem.3c02143