U-104 (SLC-0111) is a highly potent inhibitor of carbonic anhydrase (CA) targeting CA IX and CA XII, with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 exhibits notable efficacy in delaying tumor growth in mouse models[1][2].
体内研究
U-104 (19, 38 mg/kg; administered daily for 27 days) suppresses primary tumor growth in mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. Furthermore, U-104 (19 mg/kg; administered daily for 5 days) inhibits the formation of metastases in the 4T1 experimental metastasis mouse model[1].
U-104 (38 mg/kg; i.p.; from 11 to 27 days) markedly retards primary tumor growth and diminishes the population of cancer stem cells in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells[2].
U-104 (50 mg/kg; oral gavage; continuously for 4 days and suspended for 1 day; from 10 to 30 days) exhibits a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells[2].
体外研究
U-104 (SLC-0111) is a highly effective inhibitor of exosomes[3].
U-104 exhibits low inhibition against CA I (Ki=5080 nM) and CA II (Ki=9640 nM)[1].
U-104 (50 μM; for 72 hours) inhibits the mesenchymal phenotype within the cancer stem cell population under hypoxic conditions in 4T1 cells. Additionally, U-104 (<50 μM) notably decreases migration in a dose-dependent manner in metastatic MDA-MB-231 LM2-4Luc+ cells, resulting in cell growth forming compact colonies resembling parental MDA-MB-231 cells[2].
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