Drug intelligence / Profile preview

7-RH

Development stage
Preclinical
Lead developer
Guangzhou Institutes of Biomedicine and Health
Modality
Small Molecules
Administration
Oral
01

Overview

7-RH (also known as 7rh or DDR1-IN-2) is a potent, selective, and orally bioavailable small-molecule inhibitor of discoidin domain receptor 1 (DDR1) with an IC50 of approximately 6.8 nM. It was discovered by researchers at the Guangzhou Institutes of Biomedicine and Health (GIBH), Chinese Academy of Sciences. 7-RH acts as an ATP-competitive kinase inhibitor, showing high selectivity for DDR1 over DDR2, Bcr-Abl, and c-Kit. In preclinical studies, 7-RH has demonstrated efficacy in suppressing cancer cell proliferation, invasion, adhesion, and tumorigenicity in various models, including pancreatic ductal adenocarcinoma (PDA), non-small cell lung cancer (NSCLC), nasopharyngeal carcinoma, and gastric cancer. Additionally, it has been investigated for its potential to delay intervertebral disc degeneration (IDD) by reducing cellular senescence and apoptosis in nucleus pulposus cells.

Other names
4-ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-benzamideDDR1 Inhibitor 2DDR-1 Inhibitor 2DDR 1 Inhibitor 2DDR1 Inhibitor 7rhDDR-1 Inhibitor 7rhDDR 1 Inhibitor 7rh
02

Targets

DDR1 (Discoidin domain receptor 1)

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