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Bleomycin Sulfate

现货
Catalog No.
A8331
化疗剂,诱发DNA链断裂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,500.00
现货
10mg
¥ 1,190.00
现货
50mg
¥ 4,690.00
现货

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Background

Bleomycin sulfate (BLENOXANE®) is a mixture of cytotoxic glycopeptide antibiotics produced by a strain of streptomyces verticillus. This component is known to cause single and/ or double-stranded breaks in DNA through approximating metals and coordinate dioxygen to generate the active species.

Bleomycin sulfate treatment resulted in elongation of E. coli cells and enlargement of HeLa cells through inhibiting DNA and protein syntheses [1].

This component is widely used in the treatment of Hodgkin's lymphoma in combination with doxorubicin, testicular cancer, squamous cell carcinomas, pulmonary fiborosis as well as in the treatment of plantar warts. For instance, Bleomycin sulfate was also shown to have

moderate to marked effects upon Rous sarcoma virus induced mouse ascites sarcoma, particularly when F1 hybrid mice were employed as host animals [2]. In addition, recent studies support the role of the proinflammatory cytokines IL-18 and IL-1beta in the mechanism of bleomycin sulfate –induced human and mouse lung injury [3].

References:
1.  Suzuki H, Nagai K, Yamaki H, Tanaka N, Umezawa H. Mechanism of action of bleomycin. Studies with the growing culture of bacterial and tumor cells. J Antibiot (Tokyo) 1968,21:379-386.
2.  Takeuchi M, Yamamoto T. Effects of bleomycin on transplantable mouse tumors. J Antibiot (Tokyo) 1968,21:631-637.
3.  Hoshino T, Okamoto M, Sakazaki Y, Kato S, Young HA, Aizawa H. Role of proinflammatory cytokines IL-18 and IL-1beta in bleomycin-induced lung injury in humans and mice. Am J Respir Cell Mol Biol 2009,41:661-670.

文献引用

1. Thompson PJ, Shah A, et al. "Targeted Elimination of Senescent Beta Cells Prevents Type 1 Diabetes." Cell Metab. 2019 Feb 14. pii: S1550-4131(19)30021-X. PMID:30799288

Chemical Properties

Physical AppearanceA solid
StorageStore at -20° C
M.Wt1512.6
Cas No.9041-93-4
FormulaC55H85N17O25S4
SynonymsBlenoxane;Bleo;Blexane
Solubility≥125 mg/mL in DMSO with gentle warming, ≥151.3 mg/mL in H2O with ultrasonic, <7.45 mg/mL in EtOH
Chemical Name3-[[2-[2-[2-[[(2R,3R)-2-[[(2R,3R,4S)-4-[[(2S)-2-[[6-amino-2-[(1S)-3-amino-1-[[(2R)-2,3-diamino-3-oxopropyl]amino]-3-oxopropyl]-5-methylpyrimidine-4-carbonyl]amino]-3-[(2S,3R,4R,5R,6R)-3-[(2R,3S,4S,5R,6R)-4-carbamoyloxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-
SDFDownload SDF
Canonical SMILESCC1=C(N=C(N=C1N)C(CC(=O)N)NCC(C(=O)N)N)C(=O)NC(C(C2=CN=CN2)OC3C(C(C(C(O3)CO)O)O)OC4C(C(C(C(O4)CO)O)OC4C(C(C(C(O4)CO)O)OC(=O)N)O)C(=O)NC(C)C(C(C)C(=O)NC(C(C)O)C(=O)NCCC5=NC(=CS5)C6=NC(=CS6)C(=O)NCCC[S+](C)C)O.OS(=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

ADIPO-P2细胞

制备方法

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 °C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 °C可放置数月。

反应条件

2.5 μg/mL;30分钟

实验结果

在ADENO-P2细胞中,Bleomycin Sulfate具有明显的致瘤作用。停药后,上述作用仍能维持至少10天。

动物实验 [2]:

动物模型

CD-1小鼠

给药剂量

5 mg/kg,2 ml/kg,气管内给药

实验结果

Bleomycin Sulfate促进炎症发展,导致严重肺纤维化,同时增加TGF-β1、Smad3和STAT1的量。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Paviolo NS, Quiroga IY, Castrogiovanni DC, Bianchi MS, Bolzán AD. Telomere instability is present in the progeny of mammalian cells exposed to bleomycin. Mutat Res. 2012 Jun 1;734(1-2):5-11.

[2]. Shi K, Jiang J, Ma T, Xie J, Duan L, Chen R, Song P, Yu Z, Liu C, Zhu Q, Zheng J. Dexamethasone attenuates bleomycin-induced lung fibrosis in mice through TGF-β, Smad3 and JAK-STAT pathway. Int J Clin Exp Med. 2014 Sep 15;7(9):2645-50.

生物活性

描述 Bleomycin sulfate是一种糖肽类抗生素,也是鳞状细胞癌(SCC)的抗癌剂,在UT-SCC-19A细胞中IC50值为4 nM。
靶点 UT-SCC-129 cells          
IC50 4 nM          

质量控制

化学结构

Bleomycin Sulfate

相关生物数据

Bleomycin Sulfate

相关生物数据

Bleomycin Sulfate

相关生物数据

Bleomycin Sulfate