U-104 (MST-104, NSC 213841, SLC-0111, WBI-5111) is a potent carbonic anhydrase (CA) inhibitor for CA IX andCA XIIwithKiof 45.1 nM and 4.5 nM, respectively, very low inhibition for CA I and CA II. In vitro
U-104 (50 \u2009μM) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 \u2009μM) 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. U-104 possesses aromatic groups at the second nitrogen ureido group.
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\u2009mg/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\u2009mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells. Cell Data
