GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC 50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer , breast cancer , and relapsed/metastatic nasopharyngeal carcinoma.
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