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  1. Metabolic Enzyme/Protease
  2. Carbonic Anhydrase
  3. CAIX Inhibitor S4

CAIX Inhibitor S4 是一種有效和選擇性的碳酸酐酶 IX/XII (CA IX/XII) 的抑制劑,Ki 值分別為 7 nM 和 2 nM。CAIX Inhibitor S4 還抑制 CA IICA I (Ki=546 nM, 5600 nM)。CAIX Inhibitor S4 可以抑制原位 MDA-MB-231 小鼠模型中肺轉(zhuǎn)移的數(shù)量,而不影響原發(fā)腫瘤的生長。

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CAIX Inhibitor S4 Chemical Structure

CAIX Inhibitor S4 Chemical Structure

CAS No. : 1330061-67-0

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10 mM * 1 mL in DMSO ¥770
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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 Carbonic Anhydrase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

CA Ⅸ

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
> 1000 μM
Compound: 9A, S4
Cytotoxicity against human HCT116 cells preincubated for 24 hrs followed by compound washout measured after 96 hrs by MTT assay
Cytotoxicity against human HCT116 cells preincubated for 24 hrs followed by compound washout measured after 96 hrs by MTT assay
[PMID: 22621623]
HT-29 IC50
20 μM
Compound: 9A, S4
Cytotoxicity against human HT-29 cells preincubated for 24 hrs followed by compound washout measured after 96 hrs by MTT assay
Cytotoxicity against human HT-29 cells preincubated for 24 hrs followed by compound washout measured after 96 hrs by MTT assay
[PMID: 22621623]
MDA-MB-231 IC50
481 μM
Compound: 9A, S4
Cytotoxicity against EGFP tagged human MDA-MB-231 cells expressing CA9 preincubated for 24 hrs followed by compound washout measured after 96 hrs by MTT assay
Cytotoxicity against EGFP tagged human MDA-MB-231 cells expressing CA9 preincubated for 24 hrs followed by compound washout measured after 96 hrs by MTT assay
[PMID: 22621623]
體外研究
(In Vitro)

CAIX Inhibitor S4 (1-100 μM;24 h) 以劑量依賴性方式抑制 MDA-MB-231、HCT116 和 HT29 細(xì)胞的增殖[1]
CAIX Inhibitor S4 (3.3-33 μM;24 h) 以濃度依賴性方式抑制 eGFP-MDA-MB-231 細(xì)胞在缺氧條件下的遷移[1]。
CAIX Inhibitor S4 (33 μM;24 h) 15-60 分鐘) 延遲 MDA-MB-231 細(xì)胞在缺氧條件下的細(xì)胞擴(kuò)散,但在常氧條件下基本上不會[1]

MCE 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.
體內(nèi)研究
(In Vivo)

CAIX Inhibitor S4 (10 mg/kg;腹腔注射 14 天) 抑制 MDA-MB-231 模型中的轉(zhuǎn)移性腫瘤負(fù)荷,同時對原發(fā)性腫瘤生長或小鼠狀況沒有影響[1]。

MCE 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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 250 mg/mL (745.42 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.9817 mL 14.9085 mL 29.8169 mL
5 mM 0.5963 mL 2.9817 mL 5.9634 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9817 mL 14.9085 mL 29.8169 mL 74.5423 mL
5 mM 0.5963 mL 2.9817 mL 5.9634 mL 14.9085 mL
10 mM 0.2982 mL 1.4908 mL 2.9817 mL 7.4542 mL
15 mM 0.1988 mL 0.9939 mL 1.9878 mL 4.9695 mL
20 mM 0.1491 mL 0.7454 mL 1.4908 mL 3.7271 mL
25 mM 0.1193 mL 0.5963 mL 1.1927 mL 2.9817 mL
30 mM 0.0994 mL 0.4969 mL 0.9939 mL 2.4847 mL
40 mM 0.0745 mL 0.3727 mL 0.7454 mL 1.8636 mL
50 mM 0.0596 mL 0.2982 mL 0.5963 mL 1.4908 mL
60 mM 0.0497 mL 0.2485 mL 0.4969 mL 1.2424 mL
80 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9318 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7454 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
CAIX Inhibitor S4
目錄號:
HY-110243
需求量: