| 产品描述: | 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 |
| 靶点: |
Ki: 2 nM (CA XII), 7 nM (CA IX), 546 nM (CA II), 5600 nM (CA I);CarbonicAnhydrase |
| 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. Cell Proliferation Assay Cell Line: MDA-MB-231, HCT116 and HT29 cells Concentration: 1, 10, 100 μM Incubation Time: 24 hours Result: Inhibited the cell proliferation of MDA-MB-231, HCT116 and HT29 cells, with IC50s of 481 μM, >1000 μM, and 20 μM, respectively. |
| 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. |
| 参考文献: |
1. Gieling RG, et, al. Antimetastatic effect of sulfamate carbonic anhydrase IX inhibitors in breast carcinoma xenografts. J Med Chem. 2012 Jun 14;55(11):5591-600. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.982 ml |
14.909 ml |
29.817 ml |
| 5 mM |
0.596 ml |
2.982 ml |
5.963 ml |
| 10 mM |
0.298 ml |
1.491 ml |
2.982 ml |
| 50 mM |
0.06 ml |
0.298 ml |
0.596 ml |
|
| 注意: |
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