Bleomycin sulfate(Synonyms: 硫酸博来霉素)

天然产物 糖类和糖苷 Saccharides and Glycosides

Bleomycin sulfate;(Synonyms: 硫酸博来霉素) 纯度: 99.60%

Bleomycin sulfate 是一种 DNA 损伤剂,抑制 DNA 合成。Bleomycin sulfate 是一种抗肿瘤抗生素 (antibiotic)。

Bleomycin sulfate(Synonyms: 硫酸博来霉素)

Bleomycin sulfate Chemical Structure

CAS No. : 9041-93-4

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10;mM;*;1 mL in DMSO ¥2166 In-stock
10 mg ¥1302 In-stock
50 mg ¥5208 In-stock
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生物活性

Bleomycin sulfate is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin sulfate is an antitumor antibiotic[1].

IC50 Target

DNA/RNA Synthesis[1]

体外研究
(In Vitro)

Bleomycin (BLM) sulfate is chosen as the best-studied micronucleus (MN) inducers in human lymphocytes with different mechanisms of genotoxicity. The most frequent Bleomycin-induced DNA lesions are single and double strand breaks and single apuinic/apyrimidinic sites. At the same time Bleomycin is true radiomimetic compound, resembling almost completely the genetic effect of ionizing radiation[1].
The IC50 value of Bleomycin sulfate for UT-SCC-19A cell line is 4.0±1.3 nM. UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin (BLM); IC50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively[2].
Bleomycin sulfate (50, 100 μM; for 24, 48 h) induce pulmonary fibrosis in RLE-6TN cell (50 μM) and A549 cell (100 μM)[4].

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

体内研究
(In Vivo)

Bleomycin sulfate treatment (3.5-4.0 mg/kg; intra-tracheal) on day 0, body weights decreases by day 4 then increases by Day 7 through the end of the study[3].
Bleomycin sulfate (3.5-4.0 mg/kg; intra-tracheal) produces a statistically significant increase in lung hydroxyproline levels, and also increases right caudal lung lobe mass[3].
Bleomycin sulfate (intratracheal instillation; 5.0 mg/kg/day) induces pulmonary fibrosis in eighty 8-week-old male BALB/c mice with weight about 20-30 g. Bleomycin induces the expression levels of α-SMA and collagen I[4].
Bleomycin sulfate (intratracheally; 2.5 mg/kg; 1.25 mg/ml, approximately 50 µl per mouse) induces pulmonary fibrosis in male C57BL/6 mice (8 weeks old, average weight approximately 24.5 g)[5].

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

Animal Model: Male Fischer 344 rats, 8-10 week old, weighing 150-250 g[3]
Dosage: 3.5-4 mg/kg
Administration: Intra-tracheal
Result: Body weights decreased by day 4 then increased by Day 7 through the end of the study.

Clinical Trial

分子量

1512.62

Formula

C55H85N17O25S4

CAS 号

9041-93-4

中文名称

硫酸博来霉素;硫酸博莱霉素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4deg;C, sealed storage, away from moisture

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 255 mg/mL (168.58 mM; Need ultrasonic and warming)

DMSO : 62.5 mg/mL (41.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6611 mL 3.3055 mL 6.6110 mL
5 mM 0.1322 mL 0.6611 mL 1.3222 mL
10 mM 0.0661 mL 0.3306 mL 0.6611 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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 (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:;Saline

    Solubility: 100 mg/mL (66.11 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (1.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.38 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (1.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.38 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (1.38 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.38 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Hovhannisyan G, et al. Comparative analysis of individual chromosome involvement in micronuclei induced by bleomycin in human leukocytes. Mol Cytogenet. 2016 Jun 21;9:49.

    [2]. Jaaskela-Saari HA, et al. Squamous cell cancer cell lines: sensitivity to bleomycin and suitability for animal xenograft studies. Acta Otolaryngol Suppl. 1997;529:241-4.

    [3]. Corboz MR, et al. Therapeutic administration of inhaled INS1009, a treprostinil prodrug formulation, inhibits bleomycin-induced pulmonary fibrosis in rats. Pulm Pharmacol Ther. 2018 Apr;49:95-103.

    [4]. Ling Peng, et al. Scutellarin ameliorates pulmonary fibrosis through inhibiting NF-κB/NLRP3-mediated epithelial-mesenchymal transition and inflammation. Cell Death Dis. 2020 Nov 13;11(11):978.

    [5]. Kang Miao, et al. Scutellarein inhibits BLM-mediated pulmonary fibrosis by affecting fibroblast differentiation, proliferation, and apoptosis. Ther Adv Chronic Dis. 2020 Jul 30;11:2040622320940185.