CAIX Inhibitor S4 is a potent, selective inhibitor of CA IX/XII with Ki values of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki of 546 nM and 5600 nM, respectively). CAIX Inhibitor S4 inhibits orthotopic MDA-MB-231 mouse model of the number of lung metastases without affecting primary tumour growth. In the concentration range of 1-100 μM for 24 h, CAIX Inhibitor S4 inhibited the proliferation of MDA-MB-231, HCT116 and HT29 cells in a dose-dependent manner. While in the concentration range of 3.3-33 μM, CAIX Inhibitor S4 inhibited the migration of eGFP-MDA-MB-231 cells under hypoxia in a concentration-dependent manner. At a concentration of 33 μM for 15-60 minutes, CAIX Inhibitor S4 retarded the spreading of MDA-MB-231 cells in hypoxia, but essentially not in normoxia[1].
CAIX Inhibitor S4 动物研究
Animal study
At a dose of 10 mg/kg administered intraperitoneally for 14 days, CAIX Inhibitor S4 inhibited metastatic tumour load in the MDA-MB-231 model, but had no effect on primary tumour growth or the condition of the mice[1].
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