Amrubicin|110267-81-7|-陌孚医药/Medlife

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Amrubicin

目录号: PC10313 纯度: ≥98%

CAS No. :110267-81-7

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中文名称

Amrubicin

中文别名

氨柔比星

英文名称

Amrubicin

英文别名

5,12-Naphthacenedione,9-acetyl-9-amino-7-[(2-deoxy-b-D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxy-,(7S,9S)-;Amrubicin;5,12-Naphthacenedione,9-acetyl-9-amino-7-[(2-deoxy-b-D-erythro-pentopyranosyl)oxy]-7,8,9,10-te...;5,12-Naphthacenedione,9-acetyl-9-amino-7-[(2-deoxy-b-D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxy-,(7S,9S;AMR;(7S,9S)-9-Acetyl-9-amino-7-[(2-deoxy--D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-naphthacenedione;5,12-Naphthacenedione,9-acetyl-9-aMino-7-(2-deoxy-b-D-erythro-pentopyranosyl)oxy-7,8,9,10-tetrahydro-6,11-dihydroxy-,(7S,9S);Amurubicin;(7S)-9β-Amino-9-acetyl-7β-[(2-deoxy-β-D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxynaphthacene-5,12-dione;5,12-Naphthacenedione,9-acetyl-9-aMino-7-(2-deoxy-b-D-erythro-pentopyranosyl)oxy-7,8,9,10-tetrahydro-6,11-dihydroxy-,(7S,9S)-;(7S,9S)-9-Amino-9-acetyl-7-[(2-deoxy-β-D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxynaphthacene-5,12-dione;(7S,9S)-9-Acetyl-9-amino-7-(2-deoxy-β-D-erythro-pentopyranosyloxy)-6,11-dihydroxy-5,7,8,9,10,12-hexahydro-5,12-naphthacenedione

Cas No.

110267-81-7

分子式

C₂₅H₂₅NO₉

分子量

483.47

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor, used for the research of cancer.

性状

Solid

IC50 & Target[1][2]

Topoisomerase II

体外研究(In Vitro)

Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor. Amrubicin (SM-5887) (2.5 μg/mL) shows radio-enhancement effects on human lung adenocarcinoma A549 cells. Amrubicin supresses the LX-1, A549, A431, and BT-474 cell lines, with IC₅₀s of 1.1 ± 0.2, 2.4 ± 0.8, 0.61 ± 0.10 and 3.0 ± 0.3 μg/mL, respectively. Amrubicin inhibits the cell cycle profile of U937 cells with an IC₅₀ of 5.6 μM. Amrubicin (SM-5887) (20 μM) also induces apoptosis in U937 cells, activates caspase-3/7 and reduces the mitochondrial membrane potential (Δψm).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Amrubicin (SM-5887) (25 mg/kg, i.v.) exhibits significant antitumor activities against both SCLC tumors, Lu-24 and Lu-134, with T/C-values (comparing the mean tumor growth rates of the treated group with those of the control group for each day that the tumors are measured) at day 14 of 17% and 9%, respectively. Amrubicin (SM-5887) (25 mg/kg, i.v.) in combination with cisplatin and irinotecan significantly inhibits the growth of tumors compared to amrubicin alone in mice bearing LX-1 tumor cells. Amrubicin (SM-5887) alone or combined with tegafur and uracil also suppresses tumor growth in human cancer xenograft models.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Hayashi S, et al. Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction. Int J Mol Med. 2006 Nov;18(5):909-15. [Information]

[2]. Hanada M, et al. Amrubicin, a novel 9-aminoanthracycline, enhances the antitumor activity of chemotherapeutic agents against human cancer cells 体外研究 and in vivo. Cancer Sci. 2007 Mar;98(3):447-54. [Information]

[3]. Hanada M, et al. Amrubicin induces apoptosis in human tumor cells mediated by the activation of caspase-3/7 preceding a loss of mitochondrial membrane potential. Cancer Sci. 2006 Dec;97(12):1396-403. Epub 2006 Sep 21. [Information]

溶解度数据

体外研究:

DMSO : ≥ 30 mg/mL (62.05 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0684 mL	10.3419 mL	20.6838 mL
5 mM	0.4137 mL	2.0684 mL	4.1368 mL
10 mM	0.2068 mL	1.0342 mL	2.0684 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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