| Description |
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, respectively, very low inhibition for CA I and CA II. |
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Targets
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| CAXII [1] |
CAIX [1] |
CAI [1] |
CAII [1] |
| 4.5 nM(Ki) |
45.1 nM(Ki) |
5.08 μM(Ki) |
9.64 μM(Ki) |
|
| 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. [2] U-104 possesses aromatic groups at the second nitrogen ureido group. [3]
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| 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. [1] 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. [2]
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COA
HPLC