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CSF1R-IN-3 is an orally effective CSF-1R inhibitor with an IC50 value of 2.1 nM. CSF1R-IN-3 has anti-proliferative activity against colorectal cancer cells. CSF1R-IN-3 exhibits anti-tumour effects and immune enhancing effects by inhibiting the migration of macrophages and inducing the reprogramming of M2-type macrophages to M1-type macrophages, thus exhibited activity against colorectal cancer cells.