Drug intelligence / Profile preview

compound 9g

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 9g is a small molecule research compound that functions as a potent inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK), also known as PDZ-binding kinase (PBK). Chemically classified as a 1-phenyl phenanthridin-6(5H)-one derivative, it targets the serine-threonine kinase TOPK, which is frequently overexpressed in various malignancies and plays a critical role in cell cycle progression and tumor growth. In preclinical models of colorectal cancer, compound 9g has demonstrated significant anti-tumor activity, showing higher potency than the known TOPK inhibitor OTS964. Pharmacokinetic evaluations in rats indicate that the compound possesses favorable drug-like characteristics, including moderate systemic clearance, a high volume of distribution, and effective oral bioavailability. Additionally, the name "compound 9g" is used in other medicinal chemistry contexts to describe different scaffolds, such as 1,2,3-triazole-incorporated 1,3,4-oxadiazole-triazine derivatives being investigated for prostate and lung cancers.

02

Targets

BRS3 (Bombesin receptor subtype 3)

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