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Daun02

现货
Catalog No.
A3352
细胞活力抑制剂,DNA合成抑制剂。
组合的产品项目
规格价格库存 数量
25mg
¥ 10,020.00
现货
5mg
¥ 3,360.00
现货
10mg
¥ 5,988.00
现货

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Background

Daun02 is an inhibitor of cell viability with IC50 values of 1.5μM, 3.5μM and 0.5μM, respectively in Panc02, MCF-7 and T47-D cell lines [1].

Daun02, an anthracycline derivative, is a substrate of β-galactosidase. β-galactosidase catalyses Daun02 into daunomycin, which causes apoptotic cell death and blockade of voltagedependent calcium channels. Daun02 has been used in the study of suicide gene therapy which has thepotential to increase the selective toxicityof conventional antitumor agents. In this study, Daun02 is shown to suppress the viability of several β-gal gene transduced tumor celllinesin vitro. However, none of thetumors responded to treatment withDaun02in vivo. This mayhave been due tothe limited aqueous solubilityof the agent.Daun02 is also used to study activated neuronal ensembles in models of conditioned drug effects and relapse. The method is called Daun02 inactivation method. In the Fos–lacZ transgenic rats, the previously drug activated neurons can be inactivated through injection of the prodrug Daun02 [1,2].

References:
[1] David Farquhar, Bih Fang Pan, Mamoru Sakurai, AjitGhosh, Craig A. Mullen, J. Arly Nelson. Suicide gene therapy using E.Coliβ-galactosidase. Cancer ChemotherPharmacol.2002, 50: 65–70.
[2] Fabio C. Cruz, EisukeKoya, Danielle H. Guez-Barber, Jennifer M. Bossert,

Carl R. Lupica, YavinShaham and Bruce T. Hope.New technologies for examining the role of neuronal ensembles in drug addiction and fear.Nature Reviews/Neuroscience. 2013, 14: 743-754.

文献引用

1. Nennig SE, Fulenwider HD, et al. "Selective Lesioning of Nuclear Factor-κB Activated Cells in the Nucleus Accumbens Shell Attenuates Alcohol Place Preference." Neuropsychopharmacology. 2018 Apr;43(5):1032-1040. PMID:28901327
2. Funk D, Coen K, et al. "Role of Central Amygdala Neuronal Ensembles in Incubation of Nicotine Craving. J Neurosci." 2016 Aug 17;36(33):8612-23. PMID:27535909

Chemical Properties

StorageStore at -20°C
M.Wt884.79
Cas No.290304-24-4
FormulaC41H44N2O20
SynonymsDaun 02; Daun-02
SolubilitySoluble in DMSO
Chemical Name[3-nitro-4-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]methyl N-[(2S,3S,4S,6R)-6-[(3-acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-2,4-dihydro-1H-tetracen-1-yl)oxy]-3-hydroxy-2-methyloxan-4-yl]carbamate
SDFDownload SDF
Canonical SMILESCC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)C)O)NC(=O)OCC6=CC(=C(C=C6)OC7C(C(C(C(O7)CO)O)O)O)[N+](=O)[O-])O
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

诱导表达E.coli β-gal的Panc02、MCF-7、T47-D、PC3、DU145和LNCap细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

EC50:0.5 到 5.5 μM;24 hours

实验结果

Daun02前体药物通过β-半乳糖苷酶转化为daunomycin。它抑制Panc02、MCF-7、T47-D、PC3、DU145和LNCap肿瘤细胞的细胞活力的EC50值分别为1.5、3.5、0.5、5.0、5.5、5.0μM。

动物实验[1]:

动物模型

植入转导β-gal的Panc02细胞的雄性无胸腺BALB/c小鼠

剂量

腹膜内注射,200 mg/kg

实验结果

目前没有发现肿瘤响应于腹膜内Daun02治疗。由于化合物的水溶性有限,Daun02的剂量是测试的最高剂量。在该剂量下,动物表现出正常的身体和行为特征,体重持续增加,证明此种药物没有实验毒性,这可能是由于Daun02细胞膜渗透性较差,分布范围较小。

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] David Farquhar, Bih Fang Pan, Mamoru Sakurai, AjitGhosh, Craig A. Mullen, J. Arly Nelson. Suicide gene therapy using E.Coli β-galactosidase. Cancer ChemotherPharmacol.2002, 50: 65–70.

生物活性

描述 Daun02是细胞活力的抑制剂,在Panc02、MCF-7和T47-D细胞系中的IC50值分别为1.5 μM、3.5 μM和0.5 μM。
靶点 Panc02 MCF-7 T47-D      
IC50 1.5 μM 3.5 μM 0.5 μM      

质量控制

化学结构

Daun02

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