Cefatrizine
Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 51627-14-6
- 分子式: C18H18N6O5S2
- 分子量:462.50
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Antibiotic アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
|
β-lactam |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-436 | IC50 |
30 μM
Compound: 40
|
Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
|
[PMID: 33650861] |
体外実験
Cefatrizine (0-100 µM; 24 h) causes a remarkable anti-proliferative effect on MCF-7 and MDA-MB-436 cell growth in a dose-dependent manner[1].
Cefatrizine (30 µM; 12 h) induces ER stress in breast cancer cells[1].
Cefatrizine (12, 24, 36 h) increases level of CHOP (marker of ER stress induced apoptosis) and promotes expressions of core proteins in eEF2K-modulated ER stress pathways (Bip, p-PERK, XBP-1S and p-JNK) in MCF-7 and MDA-MB-436 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7, MDA-MB-436 cells
-
Concentration:0-100 µM
-
Incubation Time:24 h
-
Result:Led to a remarkable anti-proliferative effect on cells and resulted in almost 50% inhibition in the MCF-7 and MDA-MB-436 cells when at 33 µM and 29 µM.
-
Cell Line:MCF-7, MDA-MB-436 cells
-
Concentration:30 µM
-
Incubation Time:12 h
-
Result:Led to massive cytoplasmic vacuolization.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MaleSwiss-Webster mice (19-21 g; P. mirabilis intracystically infected model)[2].
-
Dosage:0.2, 1, 5, 25 mg/kg
-
Administration:Oral administration; 4 times daily for 3 days.
-
Result:Reduced the number of infecting organisms to less than 1,000 in the bladder when 1 mg/kg, and in the kidneys when 0.2 mg/kg.
化学情報
-
CAS 番号 51627-14-6
-
分子量 462.50
-
分子式 C18H18N6O5S2
-
SMILES
O=C(O)C(N1[C@@]([H])([C@@H](C1=O)NC([C@@H](C2=CC=C(C=C2)O)N)=O)SC3)=C3CSC4=CNN=N4
-
別名
BL-S-640; SK&F 60771
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
溶剤 & 溶解度
体外:
H2O : 250 mg/mL (540.54 mM; Need ultrasonic)
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
参考文献
[1]. Yao Z, et al. Integrative bioinformatics and proteomics-based discovery of an eEF2K inhibitor (cefatrizine) with ER stress modulation in breast cancer cells. Mol Biosyst. 2016 Mar;12(3):729-36. [Content Brief]
[2]. Leitner F, et al. BL-S640, a cephalosporin with a broad spectrum of antibacterial activity: bioavailability and therapeutic properties in rodents. Antimicrob Agents Chemother. 1975 Mar;7(3):306-10. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.1622 mL | 10.8108 mL | 21.6216 mL | 54.0541 mL |
| 5 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL | 10.8108 mL | |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL | 5.4054 mL | |
| 15 mM | 0.1441 mL | 0.7207 mL | 1.4414 mL | 3.6036 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0811 mL | 2.7027 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL | 2.1622 mL | |
| 30 mM | 0.0721 mL | 0.3604 mL | 0.7207 mL | 1.8018 mL | |
| 40 mM | 0.0541 mL | 0.2703 mL | 0.5405 mL | 1.3514 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3604 mL | 0.9009 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2703 mL | 0.6757 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.