GLPBio

Bleomycin A5 (hydrochloride)

Catalog No.: GC10909Purity:>85.00%Synonyms: Pingyangmycin
COASDSData Sheet
Bleomycin A5 (Pingyangmycin)-Hydrochlorid ist ein antineoplastisches Glykoprotein-Antibiotikum.

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Bleomycin A5 (hydrochloride)
Cas No.: 55658-47-4
5mgIn Stock
$76.00
1
10mgIn Stock
$142.00
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25mgIn Stock
$332.00
1
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Beschreibung (Description)

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.

Protokoll (Protocol)

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.

Produktdokumente (Product Documents)

Purity:>85.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
55658-47-4
Synonyme
Pingyangmycin
Chemischer Name
N1-[3-[(4-aminobutyl)amino]propyl]-bleomycinamide, hydrochloride
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@]
Summenformel
C57H89N19O21S2 • XHCl
Molekulargewicht
1477
Löslichkeit
DMSO: 0.1 mg/mL,PBS (pH 7.2): 10 mg/mL
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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