Bleomycin A5 (hydrochloride)是一种糖肽类抗生素，具有抗肿瘤活性。
Cas No.:55658-47-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Bleomycin A5 (hydrochloride) is a glycopeptide antibiotic that acts as the antitumor agent [1]. Bleomycin A5 acts on S stage of cell cycle to snip DNA chain during cell mitosis and disturb the cell proliferation[2]. Bleomycin A5 has been widely used to establish rat models of pulmonary fibrosis and to increase the serum levels of inflammatory cytokines[3].
In vitro, Bleomycin A5 treatment for 72 hours significantly inhibited the viability of nasal polyp-derived fibroblasts (NPDFs), with an IC50 value of 132μM[4]. Treatment with 15μg/ml Bleomycin A5 for 24 hours can increase the levels of caspase-3 and p53, inhibit telomerase activity, and induce apoptosis in ECV304 cells[5]. Treatment with 80μg/ml Bleomycin A5 for 24 hours can induce the expression of p21 in A549 cells, inhibit the expression and phosphorylation of EGFR, and cause cell cycle arrest[6].
In vivo, intratracheal administration of a single dose of Bleomycin A5 (5mg/kg) significantly induced lung inflammation and fibrosis in rats over a period of seven days[7].
References:
[1] Dorr R T, Meyers R, Snead K, et al. Analytical and biological inequivalence of two commercial formulations of the antitumor agent bleomycin[J]. Cancer chemotherapy and pharmacology, 1998, 42(2): 149-154.
[2] Luo Q, Zhao F. The effects of Bleomycin A5 on infantile maxillofacial haemangioma[J]. Head & face medicine, 2011, 7(1): 11.
[3] Wang A, Wang F, Yin Y, et al. Dexamethasone reduces serum level of IL-17 in Bleomycin-A5-induced rats model of pulmonary fibrosis[J]. Artificial Cells, Nanomedicine, and Biotechnology, 2018, 46(4): 783-787.
[4] Wu F, Tian P, Ma Y, et al. Induction of apoptosis in nasal polyp-derived fibroblasts by bleomycin A5 in vitro[J]. Molecular Medicine Reports, 2018, 17(4): 5384-5389.
[5] Huang Y D, Li P, Tong X, et al. Effects of bleomycin A5 on caspase-3, P53, bcl-2 expression and telomerase activity in vascular endothelial cells[J]. Indian Journal of Pharmacology, 2015, 47(1): 55-58.
[6] He Y, Lan Y, Liu Y, et al. Pingyangmycin and bleomycin share the same cytotoxicity pathway[J]. Molecules, 2016, 21(7): 862.
[7] Pan J B, Hou Y H, Zhang G J. Rolipram attenuates bleomycin A5‐induced pulmonary fibrosis in rats[J]. Respirology, 2009, 14(7): 975-982.
Bleomycin A5 (hydrochloride)是一种糖肽类抗生素，具有抗肿瘤活性[1]。Bleomycin A5作用于细胞周期的S期，在细胞有丝分裂过程中切割DNA链，干扰细胞增殖[2]。Bleomycin A5已被广泛用于建立大鼠肺纤维化模型，并用于增加血清中炎症细胞因子的水平[3]。
在体外，Bleomycin A5处理72小时显著抑制了鼻息肉来源成纤维细胞(NPDFs)的活力，IC50值为132μM[4]。使用15μg/ml的Bleomycin A5处理ECV304细胞24小时，可增加caspase-3和p53的水平，抑制端粒酶活性，并诱导细胞凋亡[5]。使用80μg/ml的Bleomycin A5处理A549细胞24小时，可诱导p21的表达，抑制EGFR的表达和磷酸化，并引起细胞周期阻滞[6]。
在体内，单次气管内给予5mg/kg的Bleomycin A5，可在七天内显著诱导大鼠肺部炎症和纤维化[7]。
| Cell experiment [1]: | |
Cell lines | Nasal polyp‑derived fibroblasts (NPDFs) |
Preparation Method | NPDFs were cultured in DMEM/F12 medium supplemented with 10% fetal bovine serum (FBS), 1% penicillin-streptomycin at 37℃ in the presence of 5% CO2. Cultured NPDFs (1×104) were seeded in each well of a 96-well plate in triplicate. After attachment, the cells were treated with Bleomycin A5 at different concentrations (0, 50, 100, 200, 300, and 400µM) for 24, 48, and 72h, then analyzed the cell viability. |
Reaction Conditions | 0, 50, 100, 200, 300, and 400µM; 24, 48, and 72h |
Applications | Bleomycin A5 treatment significantly reduced the cell viability of NPDFs in a concentration and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Male Wistar rats (200-220g) were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility with food and tap water ad libitum. Rats were administered a single dose of Bleomycin A5 (5mg/kg) intratracheally. The sham group were administered the same volume of saline intratracheally, and both groups were injected intraperitoneally with 2.5% ethanol. Day 0 was defined as the day on which Bleomycin A5 was injected. On day 7, 1ml of 10% buffered formaldehyde was perfused into the lung via an intratracheal cannula, and the whole lungs were excised and fixed in 10% buffered formaldehyde. The fixed lungs were embedded in paraffin, stained with HE and Masson's trichrome. |
Dosage form | 5mg/kg for once; intratracheal administration |
Applications | Bleomycin A5 treatment induced lung inflammation and fibrosis in rats. |
References: | |
| Cas No. | 55658-47-4 | SDF | |
| 别名 | 盐酸平阳霉素,Pingyangmycin | ||
| 化学名 | N1-[3-[(4-aminobutyl)amino]propyl]-bleomycinamide, hydrochloride | ||
| Canonical SMILES | CC(C(N1)=N)=C(N=C1[C@](NC[C@@](N)([H])C(O)=N)([H])CC(O)=N)/C(O)=N/[C@@](/C(O)=N/[C@]([C@](O)([H])[C@@](/C(O)=N/[C@@](/C(O)=N/CCC2=NC(C3=NC(/C(O)=N/CCCNCCCCN)=CS3)=CS2)([H])[C@@](O)([H])C)([H])C)([H])C)([H])[C@](O[C@@]4([H])[C@](O[C@]5([H])[C@](O)([H])[C@] | ||
| 分子式 | C57H89N19O21S2 • XHCl | 分子量 | 1477 |
| 溶解度 | DMSO: 0.1 mg/mL,PBS (pH 7.2): 10 mg/mL | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 677 μL | 3.3852 mL | 6.7705 mL |
| 5 mM | 135.4 μL | 677 μL | 1.3541 mL |
| 10 mM | 67.7 μL | 338.5 μL | 677 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >85.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet