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5mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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10 mM * 1 mL in DMSO |
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Purity: ≥98%
Bleomycin Sulfate (also known as NSC125066; NSC-125066; BLEO-cell; Bleolem; Blenoxane; Blanoxan), the sulfate salt of Bleomycin, is a glycopeptide antibiotic and an anticancer agent approved for treating a variety of cancers including Hodgkin's lymphoma, non-Hodgkin's lymphoma, ovarian cancer, testicular cancer, and cervical cancer. It exhibits strong anti-proliferative activity in vitro against a range of cancer cell lines, including squamous cell carcinomas, in UT-SCC-19A cells, where the IC50 is 4 nM. Combining the sulfate salts of basic glycopeptide antineoplastic antibiotics that were extracted from Streptomyces verticillus is bleomycin sulfate. It combines with iron to form complexes that convert molecular oxygen to superoxide and hydroxyl radicals, which damage DNA strands one way or both, as well as causing lipid peroxidation and the oxidation of carbohydrates, among other things.
Targets |
DNA/RNA Synthesis
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ln Vitro |
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ln Vivo |
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Cell Assay |
ADIPO-P2 cells are cultured in D-MEM high glucose medium at 37 °C with 5% CO2 atmosphere, supplemented with 20% fetal calf serum, penicillin (100 U/mL), and streptomycin (100 μg/mL). 1.5 × 105 cells/mL are cultured as monolayers in TC25 Corning flasks. Two flasks are set up for each experiment: one for the treated culture and one for the control. ADIPO-P2 cells are exposed to a 30-minute pulse of 2.5 μg/mL bleomycin sulfate during the log phase of growth. Parallel cultures serving as controls are not subjected to bleomycin sulfate. The duration and concentration of bleomycin sulfate exposure are selected based on earlier research using bleomycin sulfate exposure in mammalian cells conducted in our lab. The cells are maintained in culture with fresh culture medium until harvesting after being twice washed with Hank's balanced salt solution following the completion of the Bleomycin sulfate pulse treatment. After treatment, cells are kept in culture continuously for five passages or subcultures. When the cultures reach confluency (approximately 4 × 105 cells/mL of culture medium), subcultivation is performed. At the time of subcultivation, cells are collected by trypsinization, and the number of viable cells is determined by staining an aliquot of approximately 200 μL with 0.4% trypan blue. This process allows for the estimation of cell growth. Subsequently, the cells are suspended in new culture medium and added to fresh culture flasks with a density of 1 × 1055 cells/mL to continue growing. After the treatments are over, the remaining cells are either thrown away or transferred to another flask for cytogenetic analysis, which takes place 18 hours and 10 days later. Colchicine (0.1 μg/mL) is added to cell cultures in the final three hours of culture to analyze chromosomal aberrations. Standard protocols are followed when preparing chromosomes. Following harvesting, cells undergo hypotonic shock, are fixed in a 3:1 methanol:acetic acid solution, are spread out onto glass slides, and then undergo PNA-FISH processing. There are two separate experiments conducted.
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Animal Protocol |
Male Fischer 344 rats, 8-10 week old, weighing 150-250 g
3.5-4 mg/kg Intra-tracheal |
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References |
[1]. Acta Otolaryngol Suppl . 1997:529:241-4. [2]. Am J Pathol . 1989 Feb;134(2):355-63. [3]. Mol Med Rep . 2012 Jun;5(6):1481-6. [4]. Mutat Res . 2012 Jun 1;734(1-2):5-11. [5]. Stem Cell Res Ther . 2012 May 29;3(3):21. [6]. Mutat Res . 2012 Sep 18;747(2):228-33. [7]. Int J Clin Exp Med . 2014 Sep 15;7(9):2645-50. eCollection 2014. |
Molecular Formula |
C55H85N17O25S4
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Molecular Weight |
1512.62
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Exact Mass |
1511.48
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Elemental Analysis |
C, 43.67; H, 5.66; N, 15.74; O, 26.44; S, 8.48
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CAS # |
9041-93-4
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CC1=C(N=C(N=C1N)C(CC(=O)N)NCC(C(=O)N)N)C(=O)NC(C(C2=CN=CN2)O[C@H]3[C@H]([C@H]([C@@H]([C@@H](O3)CO)O)O)O[C@@H]4[C@H]([C@H]([C@@H]([C@H](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-]
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InChi Key |
WUIABRMSWOKTOF-OCBSMOPSSA-N
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InChi Code |
InChI=1S/C55H83N17O21S3.H2O4S/c1-20-33(69-46(72-44(20)58)25(12-31(57)76)64-13-24(56)45(59)82)50(86)71-35(41(26-14-61-19-65-26)91-54-43(39(80)37(78)29(15-73)90-54)92-53-40(81)42(93-55(60)88)38(79)30(16-74)89-53)51(87)66-22(3)36(77)21(2)47(83)70-34(23(4)75)49(85)63-10-8-32-67-28(18-94-32)52-68-27(17-95-52)48(84)62-9-7-11-96(5)6;1-5(2,3)4/h14,17-19,21-25,29-30,34-43,53-54,64,73-75,77-81H,7-13,15-16,56H2,1-6H3,(H13-,57,58,59,60,61,62,63,65,66,69,70,71,72,76,82,83,84,85,86,87,88);(H2,1,2,3,4)/t21?,22?,23?,24?,25?,29-,30+,34?,35?,36?,37+,38+,39-,40-,41?,42-,43-,53+,54-;/m0./s1
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Chemical Name |
3-[[2-[2-[2-[[2-[[4-[[2-[[6-amino-2-[3-amino-1-[(2,3-diamino-3-oxopropyl)amino]-3-oxopropyl]-5-methylpyrimidine-4-carbonyl]amino]-3-[(2R,3S,4S,5S,6S)-3-[(2R,3S,4S,5R,6R)-4-carbamoyloxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxy-2-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]ethyl]-1,3-thiazol-4-yl]-1,3-thiazole-4-carbonyl]amino]propyl-dimethylsulfanium;hydrogen sulfate
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Synonyms |
NSC-125066; BLEO; BLM; NSC 125066; BLEO cell; BLEO-cell; NSC125066; BLEOcell; Bleolem; Bleomycin sulfate; Trade name: Blenoxane. Blanoxan
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL Solubility in Formulation 5: 100 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Solubility in Formulation 6: 100 mg/mL (Infinity mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.6611 mL | 3.3055 mL | 6.6110 mL | |
5 mM | 0.1322 mL | 0.6611 mL | 1.3222 mL | |
10 mM | 0.0661 mL | 0.3306 mL | 0.6611 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01858922 | Active Recruiting |
Drug: ABVE-PC Drug: DECA |
Hodgkin Disease | Baylor College of Medicine | December 19, 2012 | Phase 2 |
NCT03159897 | Active Recruiting |
Drug: Doxorubicin Drug: Bleomycin |
Hodgkin Lymphoma | Fondazione Italiana Linfomi - ETS | August 1, 2017 | Phase 3 |
NCT01712490 | Active Recruiting |
Drug: bleomycin Drug: vinblastine |
Hodgkin Lymphoma | Takeda | November 9, 2012 | Phase 3 |
NCT01873326 | Active Recruiting |
Drug: Paclitaxel Drug: Bleomycin |
Germ Cell Tumors | Memorial Sloan Kettering Cancer Center |
June 2013 | Phase 2 |
NCT01347294 | Active Recruiting |
Drug: Bleomycin + Fibrovein Drug: Bleomycin |
Venous Malformation | Oslo University Hospital | August 2011 | Phase 4 |
Chromosomal content of micronuclei (MN) in binucleated human leukocytes. The MN in mitomycin C- and bleomycin-treated human leukocytes were sequentially analyzed by three-color FISH using centromeric probes (cep) and whole chromosome paints (wcp). Mol Cytogenet . 2016 Jun 21:9:49. td> |
Int J Clin Exp Med . 2014 Sep 15;7(9):2645-50. eCollection 2014. td> |
Increase in collagen content of lung post-bleomycin in gp91phox-/- but not in MM12-gp91phox double knockout mice. Stem Cell Res Ther . 2012 May 29;3(3):21. td> |
Study design of BrdU pulse chase of control and bleomycin-induced lung fibrosis model in mice. Stem Cell Res Ther . 2012 May 29;3(3):21. td> |
Cellularity in bronchoalveolar lavage fluid and lung before and after bleomycin challenge at day 7 in wildtype vs. gp91phox-/- and MMP12-gp91phox double knockout mice. Stem Cell Res Ther . 2012 May 29;3(3):21. td> |