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Bleomycin A5 (hydrochloride)

Catalog No.
C3370
glycopeptide antibiotic that lead to nucleic acid cleavage
Grouped product items
SizePriceStock Qty
5mg
$158.00
Ship with 5-10 days
10mg
$277.00
Ship with 5-10 days
25mg
$608.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Bleomycin A5 is an anticancer chemotherapeutic that binds DNA and induces DNA cleavage and strand breaks, it is highly toxic. Additionally, this compound induces apoptosis, alters cell cycle regulation, inhibits proliferation, and decreases tumor size in cellular and animal models of hemangioma. Bleomycin may also inhibit thioredoxin reductase.

In vitro: The IC50 of BLM alone to the cells was about 2.63 μg/ml. The IC50 of BLM was decreased to 1/3.8 and 1/9.5 of 2.63 μg/ml when used in combination with 2.63 μg/ml and 5 μg/ml W-131 [1]. Bleomycin A5 induced the activation of a JNK pathway in a dose-dependent manner. After 24h treatment, Bleomycin A5 induced dramatic cell death. DAPI nuclear staining assay revealed that PD98059 (10 μM) markedly enhanced bleomycin A5-induced apoptosis [2].

In vivo: In the rats, Bleomycin A5 induced pulmonary inflammation and fibrosis, increased the levels of malondialdehyde and tumour necrosis factor-α and enhanced accumulation of collagen in the lungs. Rolipram administration significantly attenuated these effects [3].

Clinical Trials: Bleomycin is clinically used to treat lymphomas, squamous cell carcinomas, and testicular cancer.

References:
[1].  Zhang H Q, He N G, Xue S B. Effect of bleomycin A5 with calmodulin inhibitor on the proliferation of S-180 cells in vitro[J]. Zhongguo yao li xue bao= Acta pharmacologica Sinica, 1990, 11(5): 470-473.
[2].  Yang L C, Yang S H, Tai K W, et al. MEK inhibition enhances bleomycin A5‐induced apoptosis in an oral cancer cell line: signaling mechanisms and therapeutic opportunities[J]. Journal of oral pathology & medicine, 2004, 33(1): 37-45.
[3].  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.

Product Citation

Chemical Properties

Physical AppearanceA powder
StorageStore at -20°C
M.Wt1477
Cas No.55658-47-4
FormulaC57H89N19O21S2·XHCl
SynonymsPingyangmycin
Solubility≤0.1mg/ml in DMSO
Chemical NameN1-[3-[(4-aminobutyl)amino]propyl]-bleomycinamide, hydrochloride
SDFDownload SDF
Canonical SMILESCC(C(N1)=N)=C(N=C1[[email protected]](NC[[email protected]@](N)([H])C(O)=N)([H])CC(O)=N)/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]]([[email protected]](O)([H])[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/CCC2=NC(C3=NC(/C(O)=N/CCCNCCCCN)=CS3)=CS2)([H])[[email protected]@](O)([H])C)([H])C)([H])C)([H])[[email protected]](O[[email protected]@]4([H])[[email protected]](O[[email protected]]5([H])[[email protected]](O)([H])[[email protected]]
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Human oral epidermoid carcinoma cell

Preparation method

The solubility of this compound in DMSO is ≤ 0.1mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

2.63 μg/ml

Applications

Bleomycin A5 induced the activation of a JNK pathway in a dose-dependent manner. After 24h treatment, Bleomycin A5 induced dramatic cell death. DAPI nuclear staining assay revealed that PD98059 (10 μM) markedly enhanced bleomycin A5-induced apoptosis.

Animal experiment [1]:

Animal models

Rat

Dosage form

5 mg/kg, intratracheal instillation

Application

In the rats, Bleomycin A5 induced pulmonary inflammation and fibrosis, increased the levels of malondialdehyde and tumour necrosis factor-α and enhanced accumulation of collagen in the lungs. Rolipram administration significantly attenuated these effects.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Yang LC, Yang SH, Tai KW, Chou MY, Yang JJ. MEK inhibition enhances bleomycin A5-induced apoptosis in an oral cancer cell line: signaling mechanisms and therapeutic opportunities. J Oral Pathol Med. 2004 Jan;33(1):37-45. PubMed PMID: 14675139.

[2]. Pan JB, Hou YH, Zhang GJ. Rolipram attenuates bleomycin A5-induced pulmonary fibrosis in rats. Respirology. 2009 Sep;14(7):975-82. doi:10.1111/j.1440-1843.2009.01606.x. PubMed PMID: 19740258.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Bleomycin A5 (hydrochloride)

Related Biological Data

Bleomycin A5 (hydrochloride)

Related Biological Data

Bleomycin A5 (hydrochloride)

Related Biological Data

Bleomycin A5 (hydrochloride)