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Busulfan

现货
Catalog No.
A8386
DNA烷化剂
组合的产品项目
规格价格库存 数量
1g
¥ 480.00
现货
5g
¥ 950.00
现货
10mM (in 1mL DMSO)
¥ 650.00
现货

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Background

Busulfan is a DNA alkylating agent [1].

DNA alkylating agent is attached to the guanine base of DNA and stops tumor growth by crosslinking guanine nucleobases in DNA double-helix strands and causes DNA damage [1].

In normal human diploid WI38 fibroblasts, busulfan (7.5-120 μM) induced senescence in a dose-dependant way, which was associated with prolonged activation of c-Jun NH2-terminal kinase (JNK), p38 mitogen-activated protein kinase (p38) and extracellular signal-regulated kinase (Erk) [2]. The induction of senescence was initiated by the transient depletion of intracellular glutathione (GSH) and then an increase in reactive oxygen species (ROS) production, which activated the Erk and p38 MAPK pathway [1].

In the adult mouse testis, busulfan induced apoptosis and decreased testis weight. In the first week, apoptosis mainly occured to spermatogonia. In the following week, spermatogonia-specific markers Stra 8 and c-kit were reduced but Gli I remained constant, which indicated apoptosis of differentiating type A spermatogonia [3].

References:
[1].  Probin V, Wang Y, Zhou D. Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway. Free Radic Biol Med, 2007, 42(12): 1858-1865.
[2].  Probin V, Wang Y, Bai A, et al. Busulfan selectively induces cellular senescence but not apoptosis in WI38 fibroblasts via a p53-independent but extracellular signal-regulated kinase-p38 mitogen-activated protein kinase-dependent mechanism. J Pharmacol Exp Ther, 2006, 319(2): 551-560.
[3].  Choi YJ, Ok DW, Kwon DN, et al. Murine male germ cell apoptosis induced by busulfan treatment correlates with loss of c-kit-expression in a Fas/FasL- and p53-independent manner. FEBS Lett, 2004, 575(1-3): 41-51.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt246.3
Cas No.55-98-1
FormulaC6H14O6S2
Solubility≥12.3mg/mL in DMSO
Chemical Name4-methylsulfonyloxybutyl methanesulfonate
SDFDownload SDF
Canonical SMILESCS(=O)(=O)OCCCCOS(=O)(=O)C
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

WI38细胞(人胚胎肺组织双倍体成纤维细胞)

溶解方法

在DMSO中的溶解度>12.3mg/mL。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

反应时间

120μM,24h

应用

Busulfan是一个烷基化剂,它可以通过交联DNA和DNA或DNA和蛋白来导致DNA损伤,在正常人二倍体WI38成纤维细胞中,Busulfan可以通过Erk(细胞外信号调节激酶)和P38 MAPK(p38丝裂原活化蛋白激酶)级联反应诱导衰老,而并不依赖于p53-DNA损伤路径。

动物实验[2]:

动物模型

8到12周的ICR雄性小鼠

剂量

药物溶解于芝麻油,40 mg/kg体重,腹腔注射

应用

Busulfan作用的小鼠表现出了显著的凋亡增加和睾丸重量下降。凋亡阳性小管百分比和凋亡细胞指数呈现出时间依赖方式的上升。Busulfan作用的小鼠中雄性生殖细胞消耗的增加是由c-kit/SCF(肝细胞因子)信号的丧失介导的,而不是p53依赖的或Fas/FasL(Fas配体)依赖的机制。

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]. Probin V, Wang Y, Zhou D. Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway. Free Radic Biol Med, 2007, 42(12): 1858-1865.

[2]. Choi YJ, Ok DW, et al. Murine male germ cell apoptosis induced by busulfan treatment correlates with loss of c-kit-expression in a Fas/FasL- and p53-independent manner. FEBS Lett, 2004, 575(1-3): 41-51.

质量控制

化学结构

Busulfan