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Bleomycin A5 (hydrochloride) (Synonyms: Pingyangmycin)

Katalog-Nr.GC10909 Copy One-Click Copy Product Info

Bleomycin A5 (Pingyangmycin)-Hydrochlorid ist ein antineoplastisches Glykoprotein-Antibiotikum.

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Bleomycin A5 (hydrochloride) Chemische Struktur

Cas No.: 55658-47-4

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Sample solution is provided at 25 µL, 10mM.



Description of Bleomycin A5 (hydrochloride)

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.

Protocol of Bleomycin A5 (hydrochloride)

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:
[1] 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.
[2] 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.

Chemical Properties of Bleomycin A5 (hydrochloride)

Cas No. 55658-47-4 SDF
Überlieferungen Pingyangmycin
Chemical Name 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@]
Formula C57H89N19O21S2 • XHCl M.Wt 1477
Löslichkeit DMSO: 0.1 mg/mL,PBS (pH 7.2): 10 mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Bleomycin A5 (hydrochloride)

Prepare stock solution
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
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