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].
U-104 细胞实验
Cell Line
Concentration
Treated Time
Description
References
4T1 murine breast cancer cells
100 µM
4-24 hours
To evaluate the effect of U-104 on the viability of 4T1 cells, results showed that U-104 did not reduce cell viability at 100 µM concentration
Am J Cancer Res. 2020 Jun 1;10(6):1761-1769.
Pt45.P1 cells
75 µM
48 hours
To evaluate the contributions by CAIX to asTF-mediated tumor progression, results showed that U-104 had no significant effect on the proliferation and mobility of Pt45.P1 cells.
Lab Invest. 2016 Dec;96(12):1234-1245.
Pt45.P1/asTF+ cells
75 µM
48 hours
To evaluate the contributions by CAIX to asTF-mediated tumor progression, results showed that U-104 significantly decreased the proliferation and mobility of Pt45.P1/asTF+ cells under hypoxic conditions.
Lab Invest. 2016 Dec;96(12):1234-1245.
MCF7 cells
50 µM
Combination treatment with ASO targeting LINC02568 and CA12 inhibitor U-104 exhibited synergistic inhibitory effects on MCF7 cell proliferation and colony formation
Adv Sci (Weinh). 2023 Sep;10(25):e2206663.
U-104 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Orthotopic pancreatic tumor model
Intraperitoneal injection
100 μl/dose
Daily for four weeks
To evaluate the inhibitory effect of U-104 on asTF-fueled tumor growth, results showed that U-104 significantly reduced the proliferation of tumor cells.
Lab Invest. 2016 Dec;96(12):1234-1245.
BALB/c-nu/nu male mice
Mouse xenograft model of human-derived pancreatic ductal adenocarcinoma cell line MIAPaCa-2
Intraperitoneal injection
20 or 40 mg/kg
Daily for 24 days
To evaluate the effect of U-104 on tumor growth, results showed that 40 mg/kg dose of U-104 significantly delayed tumor growth
Anal Chem. 2023 Feb 28;95(8):3940-3950
BALB/C nude mice
MCF7 cell xenograft model
Intraperitoneal injection
50 mg/kg
Every other day for six times
Combination treatment with ASO targeting LINC02568 and U-104 exhibited synergistic inhibitory effects on MCF7 cell-derived tumor growth
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