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U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.in vitro: U-104 (50 μM) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 μM) significantly reduces migration in a dose-dependent manner in metastatic MDA-MB-231 LM2-4Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells.
in vivo: U-104 (38 mg/kg) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg) inhibits metastases formation in the 4T1 experimental metastasis mice model. U-104 (38 mg/kg) significantly delay primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. U-104 (5 mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells. For the detailed information of U-104, the solubility of U-104 in water, the solubility of U-104 in DMSO, the solubility of U-104 in PBS buffer, the animal experiment (test) of U-104, the cell expriment (test) of U-104, the in vivo, in vitro and clinical trial test of U-104, the EC50, IC50,and affinity,of U-104, For the detailed information of U-104, the solubility of U-104 in water, the solubility of U-104 in DMSO, the solubility of U-104 in PBS buffer, the animal experiment (test) of U-104, the cell expriment (test) of U-104, the in vivo, in vitro and clinical trial test of U-104, the EC50, IC50,and affinity,of U-104, Please contact DC Chemicals. |