Bleomycin Sulfate (Synonyms: Blenoxane;Bleo;Blexane) |
| Katalog-Nr.GC15819 |
Bleomycin wird von Streptomyces verticillis produziert.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 9041-93-4
Sample solution is provided at 25 µL, 10mM.
Bleomycin is produced by Streptomyces verticillis. The Bleomycin molecule has two main structural components; a bithiazole component which partially intercalates into the DNA helix, parting the strands, as well as pyrimidine and imidazole structures, which bind iron and oxygen forming an activated complex capable of releasing damaging oxidants in close proximity to the polynucleotide chains of DNA. This may lead to chain scission or structural modifications leading to release of free bases or their propenal derivatives. It has potent tumor killing properties which have gained it an critical role in cancer chemotherapy. It causes little marrow suppression, but the major adverse is pulmonary toxicity effect.[1]
In vitro, Bleomycin reacts with DNA which has previously been treated with a sulfhydryl compound, and cause a decrease in its melting temperature (Tm). In the reactions in vitro, strand scission in DNA has been confirmed which indicate that in the presence of a sulfhydryl compound in vitro, Bleomycin binds to DNA, and causes single-strand scission. The scission of DNA may be the cause of the inhibition of thymidine incorporation into DNA of growing cells and the inhibition of cell division. [2]
In vivo study demonstrated that Bleomycin-induced pulmonary toxicity and fibrosis could be significantly affected by Soluble epoxide hydrolase (sEH) inhibitors AUDA. In vivo, AUDA significantly improved Bleomycin -induced decline in lung function and body weight, and inhibited inflammatory cell accumulation and the mRNA and protein expression of interleukin (IL)-1β, TGF-β1, and matrix metalloproteinase 9 (MMP-9) in lung tissue. [3]
References:
[1]. John H. et al. Mechanisms of Bleomycin-induced lung damage. Arch Toxicol (1991) 65:81-94.
[2]. Suzuki H, et al. On the mechanism of action of Bleomycin: scission of DNA strands in vitro and in vivo. J Antibiot (Tokyo). 1969 Sep;22(9):446-8.
[3]. Xin-wei D, et al. Soluble epoxide hydrolase inhibitor AUDA decreases Bleomycin-induced pulmonary toxicity in mice by inhibiting the p38/Smad3 pathways. Toxicology 389 (2017) 31–41.
| Cell experiment [1]: | |
|
Cell lines |
Hela cells |
|
Preparation Method |
HeLa cells, labelled with 3H~thymidine (0.05 pic/ml, 1,850 mc/mM) for 20 hours, |
|
Reaction Conditions |
Cells were incubated with bleomycin A2 (8 or 40 μg/ml) for 6 hours at 37°C. |
|
Applications |
Bleomycin can cause the single-strand scission. The sulfhydryl compound is necessary for bleomycin A2 to cause scission in DNA strand as in the case of decreasing Tm of DNA. Unless EDTA was added to the cell suspension, more marked scission of DNA was demonstrated. The enhancement of DNA degradation seemed to occur during the extraction procedure. |
| Animal experiment [2]: | |
|
Animal models |
D1CC×D1BC tg mice，bred on a DBA/1J background |
|
Preparation Method |
Bleomycin was mixed with an equal amount of microbubbles (Ultrasound Contrast Agent SV-25) and administered via the i.t. route by a spray nebulizer (40 μl/mouse, 1.28 mg/kg body weight) before sonoporation on the chest by 1.0 W/cm2 for 1 min (Sonitron GTS Sonoporation System). Mice were anesthetized with isoflurane and the chest hair was shaved for sonoporation. |
|
Dosage form |
0.512 mg/ml in normal saline |
|
Applications |
Bleomycin is most commonly used to develop pulmonary fibrosis in animal models. In animal models, administration of single or multiple doses of bleomycin by either intra-tracheal (i.t.) instillation, osmotic pump, intravenous route, or intranasal delivery induces pulmonary fibrosis, results in significant dose-dependent mortality. |
|
References: [1]. Suzuki H, et al. On the mechanism of action of bleomycin: scission of DNA strands in vitro and in vivo. J Antibiot (Tokyo). 1969 Sep;22(9):446-8. [2]. Yoko Miura, et al. Bimodal fibrosis in a novel mouse model of bleomycin-induced usual interstitial pneumonia. Life Sci Alliance. 2022 Jan; 5(1): e202101059. |
|
| Cas No. | 9041-93-4 | SDF | |
| Überlieferungen | Blenoxane;Bleo;Blexane | ||
| Chemical Name | 3-[[2-[2-[2-[[(2R,3R)-2-[[(2R,3R,4S)-4-[[(2S)-2-[[6-amino-2-[(1S)-3-amino-1-[[(2R)-2,3-diamino-3-oxopropyl]amino]-3-oxopropyl]-5-methylpyrimidine-4-carbonyl]amino]-3-[(2S,3R,4R,5R,6R)-3-[(2R,3S,4S,5R,6R)-4-carbamoyloxy-3,5-dihydroxy-6-(hydroxymethyl)oxan- | ||
| Canonical SMILES | CC1=C(N=C(N=C1N)C(CC(=O)N)NCC(C(=O)N)N)C(=O)NC(C(C2=CN=CN2)OC3C(C(C(C(O3)CO)O)O)OC4C(C(C(C(O4)CO)O)OC4C(C(C(C(O4)CO)O)OC(=O)N)O)C(=O)NC(C)C(C(C)C(=O)NC(C(C)O)C(=O)NCCC5=NC(=CS5)C6=NC(=CS6)C(=O)NCCC[S+](C)C)O.OS(=O)(=O)[O-] | ||
| Formula | C55H85N17O25S4 | M.Wt | 1512.6 |
| Löslichkeit | ≥ 125 mg/mL in DMSO with gentle warming, ≥ 151.3 mg/mL in Water with ultrasonic, <7.45 mg/mL in EtOH | Storage | Store at -20°C,sealed storage, away from moisture |
| 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. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.6611 mL | 3.3056 mL | 6.6111 mL |
| 5 mM | 0.1322 mL | 0.6611 mL | 1.3222 mL |
| 10 mM | 0.0661 mL | 0.3306 mL | 0.6611 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
Gracillin alleviates collagen deposition and pulmonary function in mice with BLM-induced PF. (A) HE staining of lung sections, 40 × magnification, scale bar: 250 μm; 200 × magnification, scale bar: 50 μm.
PF was induced in model mice via a single intratracheal BLM (3 mg/kg) (GLPBIO) instillation.
Journal of Ethnopharmacology (2023): 116704. PMID: 37257706 IF: 5.3999 -
Related Biological Data
Baicalin mitigated cell apoptosis in both bleomycin-induced pulmonary fibrosis and bleomycin-treated MLE-12; this effect was impeded by 5-HD. (C) Cell apoptosis was examined through flow cytometry.
In vitro, MLE-12 cells were treated with BLM (35 μM) (GLPBIO) for 24 h to induce cell injury.
Toxicology (2023): 153638. PMID: 37783230 IF: 4.5003 -
Related Biological Data
hESC-MSC-Exos mitigate Pt- and BLM-induced γH2AX protein level increase. (C) and (D): Quantification results of γH2AX fluorescence intensity from (A) and (B), respectively.
Consistent with previous reports, after HeLa cells were treated with 1 μMol/L Pt or 10 μMol/L BLM(GLPBIO) for 24 h, the intracellular ROS level increased robustly in comparison with the untreated group as measured by DCFH staining.
Mutat Res-Gen Tox En (2023): 503651. PMID: 37491116 IF: 1.9 -
Related Biological Data
6-Gingerol improves the survival rate of bleomycin-induced mice and reduces lung pathology. (B) The changes of lung pathology in each group were observed by H&E staining.
The mice were randomly divided into four groups: control,BLM, BLM + 6-gingerol 100 mg/kg, BLM + 6-gingerol 250 mg/kg. BLM group: for the induction of fibrosis, BLM (purity > 98.00%, GlpBio, United States) was dissolved in 50 μL sterile PBS, and mice were intratracheally administered (2 mg/kg body weight) with a single dose of BLM.
Allergol Immunopath 50.2 (2022): 104-114. PMID: 35257553 IF: 1.667
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *