| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, N,N'-(2,2'-dimethyl[1,1'-biphenyl]-3,3'-diyl)bis[5-[[(2-hydroxyethyl)amino]methyl]- | [CAS]
2368182-63-0 | [Synonyms]
ARB-272572
2-Pyridinecarboxamide, N,N'-(2,2'-dimethyl[1,1'-biphenyl]-3,3'-diyl)bis[5-[[(2-hydroxyethyl)amino]methyl]- | [Molecular Formula]
C32H36N6O4 | [MOL File]
2368182-63-0.mol | [Molecular Weight]
568.67 |
| Chemical Properties | Back Directory | [Boiling point ]
710.5±60.0 °C(Predicted) | [density ]
1.284±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
11.45±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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