Targeting Tumor Growth: The Potential of CS2164 as a Multi-Target Inhibitor in Cancer Therapy

A novel compound, CS2164, has been developed as a multi-targeted kinase inhibitor to address the limitations of current anti-cancer drugs, which include insufficient efficacy and drug resistance. This small molecule has been shown to effectively inhibit several key enzymes involved in tumor growth, including angiogenesis-related kinases such as VEGFR2, VEGFR1, VEGFR3, PDGFRα, and c-Kit, as well as mitosis-related kinase Aurora B and chronic inflammation-related kinase CSF-1R. The inhibitory concentrations (IC50) of CS2164 for these targets are in the low nanomolar range, indicating high potency.

The compound has demonstrated its anti-angiogenic properties by inhibiting VEGFR/PDGFR phosphorylation, suppressing cell proliferation, and preventing the formation of blood vessels in tumor tissues. Additionally, CS2164 induces cell cycle arrest at the G2/M phase and inhibits cell proliferation through the suppression of Aurora B-mediated H3 phosphorylation. It also affects the inflammatory process by inhibiting CSF-1R phosphorylation, leading to a reduction in monocyte-to-macrophage differentiation and a decrease in CSF-1R+ cells within tumors.

In vivo studies have shown that CS2164 can significantly reduce or completely halt tumor growth at well-tolerated oral doses in various human tumor xenograft models. These findings suggest that CS2164 is a highly selective and potent multi-kinase inhibitor with significant anti-tumor activity against tumor angiogenesis, mitosis, and chronic inflammation. This makes CS2164 a promising candidate for further clinical evaluation as a potential therapeutic agent for cancer treatment.