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编 号:F121453
分子式:C15H17N3O4S
分子量:335.38
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.

体内研究:
CAIX Inhibitor S4 (10 mg/kg; i.p. for 14 days) inhibits metastatic tumor burden in MDA-MB-231 model while having no effect on primary tumor growth or mouse condition.Animal Model:Female nu/nu CBA mice (10-12 weeks) were injected with eGFP-MDA-MB-231 cells
Dosage:10 mg/kg
Administration:I.p. daily on a “5 days on, 2 days off” dosing regimen for 14 days
Result:Significantly reduced the metastatic tumor burden in lungs of mice bearing orthotopic eGFP-MDA-MB-231 tumors.The average body weights between vehicle and S4 treated mice were similar throughout the experiments.

体外研究:
CAIX Inhibitor S4 (1-100 μM; 24 h) inhibits the proliferation of MDA-MB-231, HCT116 and HT29 cells in a dose-dependent manner.CAIX Inhibitor S4 (3.3-33 μM; 24 h) inhibits the eGFP-MDA-MB-231 cell migration in anoxia in a concentration- dependent manner.CAIX Inhibitor S4 (33 μM; 15-60 min) delays the cell spreading of MDA-MB-231 cells in anoxia but essentially not in normoxia.
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