U-104

U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with K_i values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model^[1][2]. IC50 & Target: Ki: 45.1 nM (CA IX) and 4.5 nM (CA XII)^[1]
EC50: 0.2 μM (exosome)^[3] In Vitro: U-104 (SLC-0111) is a potent exosome inhibitor^[3].
U-104 has low inhibition for CA I (K_i=5080 nM) and CA II (K_i=9640 nM)^[1].
U-104 (50 μM; for 72 hours) 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 LM2-4^Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells^[2]. In Vivo: U-104 (19, 38 mg/kg; daily; for 27 days) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg; daily; for 5 days) inhibits metastases formation in the 4T1 experimental metastasis mice model^[1].
U-104 (38 mg/kg; i.p.; from 11 to 27 days) significantly delays primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4^Luc+ cells^[2].
U-104 (50 mg/kg; oral gavage; continuously for 4 days and suspended for 1 day; from 10 to 30 days) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells^[2].