Cefatrizine (BL-S-640) 是一种口服有效的广谱头孢菌素类抗生素。Cefatrizine 也是一种eEF2K抑制剂，在人乳腺癌细胞中具有抗增殖活性，可诱导 ER 应激，导致细胞死亡。Cefatrizine 可用于癌症和细菌感染的研究。
| 生物活性 | Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporinantibiotic. Cefatrizine is also aeEF2Kinhibitor, with anti-proliferative activity in human breastcancercells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies ofcancerandbacterialinfection[1][2]. |
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体外研究
(In Vitro) | 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].
Cell Proliferation Assay[1] | 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 Viability Assay[1] | Cell Line: | MCF-7, MDA-MB-436 cells | | Concentration: | 30 μM | | Incubation Time: | 12 h | | Result: | Led to massive cytoplasmic vacuolization. |
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体内研究
(In Vivo) | Cefatrizine (BL-S-640) (0.2, 1, 5, 25 mg/kg; p.o.; 4 times daily for 3 days) reduces the number of infecting organisms in the bladder and the kidneys inP. mirabilisintracystically infected model[2].
| Animal Model: | MaleSwiss-Webster mice (19-21 g;P. mirabilisintracystically 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. |
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| 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. |
| 溶解性数据 | In Vitro: H2O : 250 mg/mL(540.54 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1622 mL | 10.8108 mL | 21.6216 mL | | 5 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL | | 10 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL |
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