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Aphidicolin
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aphidicolin图片
CAS NO: 38966-21-1
包装与价格:
包装 价格(元)
1mg 电议
5mg 电议
10mg 电议

半岛bd体育手机客户端 名称
阿非迪霉素
半岛bd体育手机客户端 介绍
Aphidicolin 是 DNA聚合酶 α 和 δ 抑制剂,通过干扰 DNA 聚合酶的活性来阻止细胞有丝分裂。Aphidicolin 是一种来源于 Cephalosporium aphidicola的抗生素, 能够抑制细胞脱氧核糖核酸合成和单纯疱疹病毒生长。Aphidicolin 具有抗正痘病毒活性,能够增强阿拉伯糖基核苷对细胞凋亡 ( apoptosis) 的诱导作用。
生物活性

Aphidicolin is an inhibitor ofDNApolymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is anantibioticproduced by moldCephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiatesapoptosisinduced by arabinosyl nucleosides in a human promyelocytic leukemia cell line[1][2][3].

体外研究
(In Vitro)

Aphidicolin (0.5 μM, 5 μM; 0-5 d) selectively kills neuroblastoma cells, but shows moderate cytotoxicity on normal human embryonal cells and HeLa, H9, A549 and Caco-2 cell lines[4].
Aphidicolin (0.4 μg/mL; 3 d) arrests cell cycle at G2 phase[5].
Aphidicolin (100 nM-10 μM; 48 h) inhibits cell proliferation via the p53-GADD45β pathway and (1 μM; 24 h) induces apoptosis in AtT-20 cells[6].
Aphidicolin (10 μM; 0-6 h) decreases the phosphorylation of Akt, (100 nM-10 μM; 24 h) increases the mRNA levels of the stress response gene growth arrest and DNA damage-inducible 45β (GADD45β), a putative downstream target of p53[6].
Aphidicolin (10 μM; 0-6 h) inhibits Varicella-zoster virus (VZV) with EC50s of 0.5-0.6 μM, with low cytotoxicity[7].

Cell Cytotoxicity Assay[4]

Cell Line: NB cell lines: UKF-NB-1/2/3 and IMR-32
Concentration: 0.5 μM, 5μM
Incubation Time: 1, 2, 3, 4, 5 days
Result: Resulted in cellular enlargement and extension of cellular processes before cell lysis occurred.

Cell Cycle Analysis[5]

Cell Line: Normal human diploid cells
Concentration: 0.4 μg/mL
Incubation Time: 3 days or 7 days
Result: Resulted more than 80% of the cells moved through S phase and were accumulated at G2 phase.
Inbihited the growth of the cells completely without causing apparent cell death.

Western Blot Analysis[6]

Cell Line: AtT-20 cells pituitary corticotroph tumor cells
Concentration: 10 μM
Incubation Time: 0 min, 5 min, 30 min, 2 h, 6 h, 24 h
Result: Inhibited Akt phosphorylation in AtT-20 cells during 5 min-2 h, in a time-dependent manner.
Increased protein level of p27 during 30 min-6 h, and remarkably increased p53 level at 24 h.
体内研究
(In Vivo)

Aphidicolin, has been developed with higher solubility agent, namely Aphidicolin glycinate (AG; NSC 303812).
Aphidicolin glycinate (100 mg/kg; i.p.; once every 3 h; 9 d) shows anti-tumor activity against the implanted B16 melanoma and M5076 sarcoma in murine, producing maximum increased life spans of 75%[8].

Animal Model: M5076 sarcoma s.c. model or B16 melanoma i.p. model in murine[8]
Dosage: 60 mg/kg, 100 mg/kg, 300 mg/kg
Administration: Intraperitoneal injection; once every 3 h; 9 days
Result: Inhibited tumor growth significantly.
分子量

338.48

性状

Solid

Formula

C20H34O4

CAS 号

38966-21-1

中文名称

阿非迪霉素

结构分类
  • Terpenoids
  • Diterpenoids
来源

Cephalosporium aphidicola

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:

DMSO : 50 mg/mL(147.72 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.9544 mL 14.7719 mL 29.5438 mL
5 mM 0.5909 mL 2.9544 mL 5.9088 mL
10 mM 0.2954 mL 1.4772 mL 2.9544 mL
*

请根据半岛bd体育手机客户端 在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的半岛bd体育手机客户端 失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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