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Fostriecin sodium salt

现货
Catalog No.
A4536
抗肿瘤抗生素
组合的产品项目
规格价格库存 数量
100ug
¥ 2,990.00
Ship with 10-15 days
500ug
¥ 9,720.00
Ship with 10-15 days

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Background

IC50: Inhibit protein phosphatase types 2A (PP2A) and 4 (PP4) intensively with an IC50 of 1.5 nM and 3 nM respectively. Inhibit topoisomerase II (Topo II) and protein phosphatase type 1 (PP1) slightly with an IC50 of 40 μM and 131 μM respectively.

Fostriecin, an anti-tumor antibiotic originates from Streptomyces pulveraceus, is considered to exert its activity by interfering the reversible phosphorylation of several important proteins in cell cycle. Fostriecin sodium salt also exhibits anti-tumor activity via suppressing enzymes including PP2A, PP4, PP1 and Topo II. [1]

In vitro: A human tumor cloning assay was adopted to investigate the antineoplastic activity of fostriecin. Variety of histologic tumor cells exposure to 10 mg/ml fostriecin resulted in 27% in vitro anticancer response. In another study using HeLa cells, by suppressing the Topo II catalytic activity, 0.22 mM fostriecin could lead to more than 90% inhibition of cancer cell DNA synthesis. [2,3]

In vivo: Fostriecin showed intensively cytotoxicity against a number of cancer cell lines and had a strong antitumor effect in animals. 10 mg/ml fostriecin could substantially suppress P388 and L1210 leukemias in mice. [2,3]

Clinical trial: Fostriecin reached clinical phase I study sponsored by the National Cancer Institute to investigate its antitumor activity in human. With dosages escalated from 2 to 20 mg/m2/day, fostriecin was administered as a 60-min intravenous (IV) infusion to 20 patients in cancer for 5 days. Although the trials were suspended due to the concerns about the storage stability of this naturally originated compound, this discovery ignited a broad interest in derivatives of fostriecin. [1,4]

References:
[1] Zhang X, Wu J, Fang L, Willis WD.  The effects of protein phosphatase inhibitors on the duration of central sensitization of rat dorsal horn neurons following injection of capsaicin. Mol Pain. 2006 Jul; 2(23). DOI:10.1186/1744-8069-2-23.
[2] Scheithauer W, Von Hoff DD, Clark G, Shillis JL, Elslager EF.  In vitro activity of the novel antitumor antibiotic fostriecin (CI-920) in a human tumor cloning assay. Eur J Cancer Res & Clin Oncol. 1986 Aug; 22(8): 921-6.
[3] Gedik CM, Collins AR.  Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells. Nnucleic Acids Res. 1990 Aug; 18(4):1008-13.
[4] Le LH, Erlichman C, Pillon L, Thiessen JJ, Day A, Wainman N, Eisenhauer EA, Moore MJ.  Phase I and pharmacokinetic study of fostriecin given as an intravenous bolus daily for five consecutive days.
Invest New Drugs.  2004 Apr; 22(2):159-67.

Chemical Properties

Physical AppearanceColourless lyophilised solid
StorageDesiccate at -20°C
M.Wt452.37
Cas No.87860-39-7
FormulaC19H26O9PNa
SolubilitySoluble in H2O
Chemical Namesodium;[(3R,4R,6R,7E,9E,11E)-3,6,13-trihydroxy-3-methyl-1-[(2R)-6-oxo-2,3-dihydropyran-2-yl]trideca-1,7,9,11-tetraen-4-yl] hydrogen phosphate
SDFDownload SDF
Canonical SMILESCC(C=CC1CC=CC(=O)O1)(C(CC(C=CC=CC=CCO)O)OP(=O)(O)[O-])O.[Na+]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HeLa细胞

溶解方法

在无菌水中的溶解度为100 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

30 min,0.22 mM

应用

Fostriecin是拓扑异构酶II的抑制剂,可抑制反应的早期阶段,并不累积损伤的DNA中间体。在人类HeLa细胞中,Fostriecin具有强效但是延时的DNA合成抑制效应。

动物实验[2]:

动物模型

皮下种植结肠38肿瘤的B6D2F1小鼠

剂量

腹腔内注射,65 mg/kg

应用

Fostriecin单剂量给药时,24小时后引起肿瘤大量坏死,Fostriecin显著诱导晚期皮下肿瘤生长延迟至少10天。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Gedik C M, Collins A R. Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells[J]. Nucleic acids research, 1990, 18(4): 1007-1013.

[2]. Baguley B C, Calveley S B, Crowe K K, et al. Comparison of the effects of flavone acetic acid, fostriecin, homoharringtonine and tumour necrosis factor α on colon 38 tumours in mice[J]. European Journal of Cancer and Clinical Oncology, 1989, 25(2): 263-269.

质量控制

质量控制和MSDS

批次:

化学结构

Fostriecin sodium salt