CAIX Inhibitor S4

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CAIX Inhibitor S4 

CAIX Inhibitor S4 是一种有效和选择性的碳酸酐酶 IX/XII (CA IX/XII) 的抑制剂，Ki 值分别为 7 nM 和 2 nM。CAIX Inhibitor S4 还抑制 CA II 和 CA I (Ki=546 nM, 5600 nM)。CAIX Inhibitor S4 可以抑制原位 MDA-MB-231 小鼠模型中肺转移的数量，而不影响原发肿瘤的生长。

CAIX Inhibitor S4

CAIX Inhibitor S4 Chemical Structure

CAS No. : 1330061-67-0

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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[1].

IC50 & Target

Ki: 2 nM (CA XII), 7 nM (CA IX), 546 nM (CA II), 5600 nM (CA I)[1]
体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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
(In Vivo)

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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nu/nu CBA mice (10-12 weeks) were injected with eGFP-MDA-MB-231 cells[1]
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.

分子量

335.38

Formula

C15H17N3O4S
CAS 号

1330061-67-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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