CAIX Inhibitor S4

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CAIX Inhibitor S4 是碳酸酐酶 IX/XII 的有效抑制剂，Ki 分别为 7 nM 和 2 nM。 CA II 和 CA I 的 Ki 分别为 546 和 5600 nM。

CAIX Inhibitor S4 is an effective inhibitor of carbonic anhydrase IX/XII with a Ki of 7 nM and 2 nM, respectively. The Kis for CA II and CA I are 546 and 5600 nM.(In Vitro):CAIX Inhibitor S4 (33 μM; 15-60 min) delays the cell spreading of MDA-MB-231 cells in anoxia but essentially not in normoxia. CAIX Inhibitor S4 (1, 10, 100 μM; 24 h) inhibits the proliferation of MDA-MB-231, HCT116 and HT29 cells in a dose-dependent manner with IC50s of 481 μM, >1000 μM, and 20 μM, respectively. CAIX Inhibitor S4 (3.3-33 μM; 24 h) inhibits the eGFP-MDA-MB-231 cell migration in anoxia in a concentration-dependent manner.(In Vivo):CAIX Inhibitor S4 (10 mg/kg; i.p.) inhibits the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.

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:24hours Result:Inhibited the cell proliferation of MDA-MB-231, HCT116 and HT29 cells, with IC50s of 481 μM, >1000 μM, and 20 μM, respectively.

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 cellsDosage: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.

S4

Membrane Transporter/Ion Channel

Carbonic Anhydrase

VEGFR2|RET

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1330061-67-0

335.38

C15H17N3O4S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (745.42 mM)

Cc1cc(C)cc(NC(=O)Nc2ccc(OS(N)(=O)=O)cc2)c1

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(-20℃)

With Ice Pack

≥ 2 years