Bleomycin hydrochloride 是一种 DNA 损伤剂,抑制 DNA 合成。Bleomycin hydrochloride 是一种抗肿瘤抗生素 (antibiotic)。
Bleomycin hydrochloride Chemical Structure
CAS No. : 67763-87-5
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10 mM * 1 mL in DMSO
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生物活性
Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic[1].
体外研究 (In Vitro)
Bleomycin hydrochloride is chosen as the best-studied micronucleus 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 hydrochloride 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; IC50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively[2]. Bleomycin hydrochloride (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 hydrochloride 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 hydrochloride (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 hydrochloride (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 hydrochloride (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
1451.00
Formula
C55H84ClN17O21S3
CAS 号
67763-87-5
中文名称
盐酸博来霉素;盐酸博莱霉素
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
H2O : 100 mg/mL (68.92 mM; Need ultrasonic)
DMSO : 50 mg/mL (34.46 mM; ultrasonic and warming and heat to 60°C)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.6892 mL
3.4459 mL
6.8918 mL
5 mM
0.1378 mL
0.6892 mL
1.3784 mL
10 mM
0.0689 mL
0.3446 mL
0.6892 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 and light)。-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:
[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 LRX-15 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.
[6]. 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.
[7]. 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.