Bleomycin sulfate | CAS#9041-93-4 | antibiotic

MedKoo Cat#: 100090 | Name: Bleomycin sulfate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus. Bleomycin exhibits potent cytotoxicity in vitro, primarily through DNA strand scission via oxidative damage induced by metal ion (Fe²⁺ or Cu²⁺)-mediated free radical formation. In various cancer cell lines, bleomycin demonstrates dose-dependent antiproliferative effects, leading to apoptosis or cell cycle arrest, often at the G2/M phase. Studies show that oxidative stress markers and DNA damage response pathways, including ATM/ATR activation, are upregulated upon treatment. Sensitivity varies by cell type, with some resistance observed due to enhanced DNA repair mechanisms or bleomycin hydrolase activity. Combination studies suggest synergistic effects with DNA-damaging agents and radiotherapy, enhancing its therapeutic potential.

Chemical Structure

Bleomycin sulfate

CAS#9041-93-4 (sulfate)

Theoretical Analysis

MedKoo Cat#: 100090

Name: Bleomycin sulfate

CAS#: 9041-93-4 (sulfate)

Chemical Formula: C55H85N17O25S4

Exact Mass: 0.0000

Molecular Weight: 1512.62

Elemental Analysis: C, 43.67; H, 5.66; N, 15.74; O, 26.44; S, 8.48

Price and Availability

Size	Price	Availability
5mg	USD 90.00	Ready to ship
10mg	USD 150.00	Ready to ship
25mg	USD 300.00	Ready to ship
50mg	USD 500.00	Ready to ship
100mg	USD 850.00	Ready to ship
200mg	USD 1,450.00	Ready to Ship

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Related CAS #

9041-93-4 (sulfate) 11056-06-7 (free base)

Synonym

BLEO; BLM; BLEO cell; BLEO-cell; BLEOcell; Bleolem; Bleomycin sulfate; US brand name: Blenoxane. Blanoxan.

IUPAC/Chemical Name

(3-(2'-((3S,6R,7S,8S,11S)-1-(6-amino-2-((S)-3-amino-1-(((S)-2,3-diamino-3-oxopropyl)amino)-3-oxopropyl)-5-methylpyrimidin-4-yl)-3-((R)-(((2R,3S,4S,5S,6S)-3-(((2R,3S,4S,5R,6R)-4-(carbamoyloxy)-3,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-4,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)(1H-imidazol-4-yl)methyl)-7-hydroxy-11-((R)-1-hydroxyethyl)-6,8-dimethyl-1,4,9,12-tetraoxo-2,5,10,13-tetraazapentadecan-15-yl)-[2,5'-bithiazole]-4-carboxamido)propyl)dimethylsulfonium hydrogensulfate

InChi Key

BRDAHBLYMDUECM-QIMPUPMHSA-N

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(26-14-61-19-66-26)91-54-43(39(80)37(78)28(16-73)90-54)92-53-40(81)42(93-55(60)88)38(79)29(17-74)89-53)51(87)67-22(3)36(77)21(2)47(83)70-34(23(4)75)49(85)63-10-8-32-65-15-30(95-32)52-68-27(18-94-52)48(84)62-9-7-11-96(5)6;1-5(2,3)4/h14-15,18-19,21-25,28-29,34-43,53-54,64,73-75,77-81H,7-13,16-17,56H2,1-6H3,(H13-,57,58,59,60,61,62,63,66,67,69,70,71,72,76,82,83,84,85,86,87,88);(H2,1,2,3,4)/t21-,22+,23+,24-,25-,28-,29+,34-,35-,36-,37+,38+,39-,40-,41-,42-,43-,53+,54-;/m0./s1

SMILES Code

C[S+](CCCNC(C1=CSC(C2=CN=C(CCNC([C@H]([C@H](O)C)NC([C@@H](C)[C@H](O)[C@@H](C)NC([C@H]([C@@H](O[C@H]3[C@@H](O[C@@H]4[C@@H](O)[C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O4)[C@@H](O)[C@H](O)[C@H](CO)O3)C5=CNC=N5)NC(C6=NC([C@@H](NC[C@H](N)C(N)=O)CC(N)=O)=NC(N)=C6C)=O)=O)=O)=O)S2)=N1)=O)C.O=S(O)([O-])=O

Appearance

Solid powder

Purity

>90% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. Bleomycin refers to a family of structurally related compounds. When used as an anticancer agent, the chemotherapeutical forms are primarily bleomycin A2 and B2. The drug is used in the treatment of Hodgkin's lymphoma (as a component of the ABVD and BEACOPP regimen), squamous cell carcinomas, and testicular cancer, as well as in the treatment of plantar warts and as a means of effecting pleurodesis. The mechanism of action involves breaking DNA. Bleomycin is on the World Health Organization's List of Essential Medicines that are needed for a basic health system. Mechanism of Action Although the exact mechanism of action of BLENOXANE is unknown, available evidence indicates that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis. Bleomycin is known to cause single, and to a lesser extent, double-stranded breaks in DNA. In in vitro and in vivo experiments, bleomycin has been shown to cause cell cycle arrest in G2 and in mitosis. When administered into the pleural cavity in the treatment of malignant pleural effusion, BLENOXANE acts as a sclerosing agent. Bleomycin sulfate Chemical Formula: C55H85N17O25S4 Molecular Weight: 1512.62 Elemental Analysis: C, 43.67; H, 5.66; N, 15.74; O, 26.44; S, 8.48 Bleomycin Chemical Formula: C55H84N17O21S3+ Exact Mass: 1414.5184 Molecular Weight: 1415.55 Elemental Analysis: C, 46.67; H, 5.98; N, 16.82; O, 23.73; S, 6.79

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#TZC51217

QC Data

View QC data: current batch, Lot#TZC51217

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Bleomycin sulfate is a DNA synthesis inhibitor.It was revealed that the number of EdU-positive cells in BLM (Bleomycin) groups was notably smaller than that in the NC group, displaying less cell proliferation, suggesting that BLM inhibits the growth of glioma cells. In addition, the levels of inflammatory factors TNF-α and INF-γ were determined, so as to detect the incidence of glioma in the early stage. It was found that the NC group had remarkably higher levels than the other two groups, while the 10 mU/ mL BLM group had obviously declined levels, suggesting that 10 mU/mL BLM can inhibit the production of inflammatory factors, further repressing the occurrence of brain glioma. These findings imply that the increased TNF-α level can further stimulate the development of brain glioma, thus aggravating the inflammatory responses. However, the level declined after the treatment with BLM, indicating that the symptoms are improved after treatment with BLM, and that BLM has favorable therapeutic effects on brain glioma. Reference: J BUON. 2020 Mar-Apr;25(2):1076-1083. https://www.jbuon.com/archive/25-2-1076.pdf

In vitro activity:

It was revealed that the number of EdU-positive cells in BLM (Bleomycin) groups was notably smaller than that in the NC group, displaying less cell proliferation, suggesting that BLM inhibits the growth of glioma cells. In addition, the levels of inflammatory factors TNF-α and INF-γ were determined, so as to detect the incidence of glioma in the early stage. It was found that the NC group had remarkably higher levels than the other two groups, while the 10 mU/ mL BLM group had obviously declined levels, suggesting that 10 mU/mL BLM can inhibit the production of inflammatory factors, further repressing the occurrence of brain glioma. These findings imply that the increased TNF-α level can further stimulate the development of brain glioma, thus aggravating the inflammatory responses. However, the level declined after the treatment with BLM, indicating that the symptoms are improved after treatment with BLM, and that BLM has favorable therapeutic effects on brain glioma. Reference: J BUON. 2020 Mar-Apr;25(2):1076-1083. https://www.jbuon.com/archive/25-2-1076.pdf

In vivo activity:

The early changes in C (day 7) and P–V loop data (CST and area, day 7) were accompanied by histological evidence of fibrotic deposition and gene expression that were apparent as early as days 7 and 14, respectively. These results are significant because they demonstrate that low-dose systemic exposure to i.p. BLM (Bleomycin) is able to induce physiological and morphological changes as early as day 7 in C57BL/6 mice and indicate that lung function is a robust and physiologically relevant tool to guide future efforts in drug discovery for IPF. Reference: Exp Physiol. 2018 Dec;103(12):1692-1703. https://physoc.onlinelibrary.wiley.com/doi/full/10.1113/EP087322

	Solvent	mg/mL	mM
Solubility
	Soluble in DMSO, not in water	0.0	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 1,512.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Jin H, Luo C. Bleomycin inhibits proliferation and promotes apoptosis of brain glioma cells via TGF-β/Smad signaling pathway. J BUON. 2020 Mar-Apr;25(2):1076-1083. PMID: 32521909. 2. Headley L, Bi W, Wilson C, Collum SD, Chavez M, Darwiche T, Mertens TCJ, Hernandez AM, Siddiqui SR, Rosenbaum S, Johnston RA, Karmouty-Quintana H. Low-dose administration of bleomycin leads to early alterations in lung mechanics. Exp Physiol. 2018 Dec;103(12):1692-1703. doi: 10.1113/EP087322. Epub 2018 Oct 17. PMID: 30260066.

In vitro protocol:

1. Jin H, Luo C. Bleomycin inhibits proliferation and promotes apoptosis of brain glioma cells via TGF-β/Smad signaling pathway. J BUON. 2020 Mar-Apr;25(2):1076-1083. PMID: 32521909.

In vivo protocol:

1. Headley L, Bi W, Wilson C, Collum SD, Chavez M, Darwiche T, Mertens TCJ, Hernandez AM, Siddiqui SR, Rosenbaum S, Johnston RA, Karmouty-Quintana H. Low-dose administration of bleomycin leads to early alterations in lung mechanics. Exp Physiol. 2018 Dec;103(12):1692-1703. doi: 10.1113/EP087322. Epub 2018 Oct 17. PMID: 30260066.

1: Russo RC, Ryffel B. The Chemokine System as a Key Regulator of Pulmonary Fibrosis: Converging Pathways in Human Idiopathic Pulmonary Fibrosis (IPF) and the Bleomycin-Induced Lung Fibrosis Model in Mice. Cells. 2024 Dec 12;13(24):2058. doi: 10.3390/cells13242058. PMID: 39768150; PMCID: PMC11674266. 2: Wang Q, Ren Z, Jin W, Jin Z. Real-world effectiveness and safety of bleomycin in patients with keloids and hypertrophic scars: a systematic review and meta- analysis. Arch Dermatol Res. 2025 Jan 6;317(1):170. doi: 10.1007/s00403-024-03687-6. PMID: 39760851; PMCID: PMC11703884. 3: Muir T, Wohlgemuth WA, Cemazar M, Bertino G, Groselj A, Ratnam LA, McCafferty I, Wildgruber M, Gebauer B, de Terlizzi F, Zanasi A, Sersa G. Current Operating Procedure (COP) for Bleomycin ElectroScleroTherapy (BEST) of low-flow vascular malformations. Radiol Oncol. 2024 Nov 28;58(4):469-479. doi: 10.2478/raon-2024-0061. PMID: 39608012; PMCID: PMC11604259. 4: Barrett A, Shah N, Chadwick A, Burns D, Burton C, Cutter DJ, Follows GA, McKay P, Osborne W, Phillips E, Wilson MR, Collins GP. Assessment of fitness for bleomycin use and management of bleomycin pulmonary toxicity in patients with classical Hodgkin lymphoma: A British Society for Haematology Good Practice Paper. Br J Haematol. 2025 Jan;206(1):74-85. doi: 10.1111/bjh.19840. Epub 2024 Nov 6. PMID: 39506502. 5: de Almeida AL, Fortuna A, Sousa M, Sá R. A systematic review of bleomycin- induced gonadotoxicity: Mechanistic implications for male reproductive health and fertility. Reprod Toxicol. 2024 Dec;130:108721. doi: 10.1016/j.reprotox.2024.108721. Epub 2024 Sep 24. PMID: 39326549. 6: You SJ, Li S, Hu CM, Zhong FY, Gan SH, Cai Y, Xiang XY. Safety and efficacy of intralesional bleomycin for keloids and hypertrophic scars: A systematic review and meta-analysis. J Cosmet Dermatol. 2024 Nov;23(11):3444-3455. doi: 10.1111/jocd.16447. Epub 2024 Aug 28. PMID: 39205503. 7: Mohammed SM, Al-Saedi HFS, Mohammed AQ, Amir AA, Radi UK, Sattar R, Ahmad I, Ramadan MF, Alshahrani MY, Balasim HM, Alawadi A. Mechanisms of Bleomycin- induced Lung Fibrosis: A Review of Therapeutic Targets and Approaches. Cell Biochem Biophys. 2024 Sep;82(3):1845-1870. doi: 10.1007/s12013-024-01384-9. Epub 2024 Jul 2. PMID: 38955925. 8: Gülle S, Çelik A, Birlik M, Yılmaz O. Skin and lung fibrosis induced by bleomycin in mice: a systematic review. Reumatismo. 2024 Mar 22;76(1). doi: 10.4081/reumatismo.2024.1642. PMID: 38523580. 9: Kim S, Woo YR, Cho SH, Lee JD, Kim HS. Clinical Efficacy of 5-Fluorouracil and Bleomycin in Dermatology. J Clin Med. 2024 Jan 6;13(2):335. doi: 10.3390/jcm13020335. PMID: 38256469; PMCID: PMC10816055. 10: Vats A, Chaturvedi P. The Regenerative Power of Stem Cells: Treating Bleomycin-Induced Lung Fibrosis. Stem Cells Cloning. 2023 Sep 12;16:43-59. doi: 10.2147/SCCAA.S419474. PMID: 37719787; PMCID: PMC10505024. 11: Sun J, Wang C, Li J, Song D, Guo L. The efficacy of bleomycin sclerotherapy in the treatment of lymphatic malformations: a review and meta-analysis. Braz J Otorhinolaryngol. 2023 Jul-Aug;89(4):101285. doi: 10.1016/j.bjorl.2023.101285. Epub 2023 Jun 29. PMID: 37423005; PMCID: PMC10344707. 12: Muir T, Bertino G, Groselj A, Ratnam L, Kis E, Odili J, McCafferty I, Wohlgemuth WA, Cemazar M, Krt A, Bosnjak M, Zanasi A, Battista M, de Terlizzi F, Campana LG, Sersa G. Bleomycin electrosclerotherapy (BEST) for the treatment of vascular malformations. An International Network for Sharing Practices on Electrochemotherapy (InspECT) study group report. Radiol Oncol. 2023 Jun 21;57(2):141-149. doi: 10.2478/raon-2023-0029. PMID: 37341196; PMCID: PMC10286891. 13: Ayilya BL, Balde A, Ramya M, Benjakul S, Kim SK, Nazeer RA. Insights on the mechanism of bleomycin to induce lung injury and associated in vivo models: A review. Int Immunopharmacol. 2023 Aug;121:110493. doi: 10.1016/j.intimp.2023.110493. Epub 2023 Jun 16. PMID: 37331299. 14: Ishida Y, Kuninaka Y, Mukaida N, Kondo T. Immune Mechanisms of Pulmonary Fibrosis with Bleomycin. Int J Mol Sci. 2023 Feb 5;24(4):3149. doi: 10.3390/ijms24043149. PMID: 36834561; PMCID: PMC9958859. 15: Seyran M, Melanie S, Philip S, Amiq G, Fabian B. Allies or enemies? The effect of regulatory T cells and related T lymphocytes on the profibrotic environment in bleomycin-injured lung mouse models. Clin Exp Med. 2023 Aug;23(4):1075-1088. doi: 10.1007/s10238-022-00945-7. Epub 2022 Nov 20. PMID: 36403186; PMCID: PMC10390389. 16: Mahdi Seyedzadeh Sani S, Sahranavard M, Jannati Yazdanabad M, Seddigh Shamsi M, Elyasi S, Hooshang Mohammadpour A, Sathyapalan T, Arasteh O, Ghavami V, Sahebkar A. The effect of concomitant use of Colony-Stimulating factors on bleomycin pulmonary toxicity - A systematic review and meta-analysis. Int Immunopharmacol. 2022 Nov;112:109227. doi: 10.1016/j.intimp.2022.109227. Epub 2022 Sep 10. PMID: 36099787. 17: Bastrup FA, Vissing M, Gehl J. Electrochemotherapy with intravenous bleomycin for patients with cutaneous malignancies, across tumour histology: a systematic review. Acta Oncol. 2022 Sep;61(9):1093-1104. doi: 10.1080/0284186X.2022.2110385. Epub 2022 Aug 27. PMID: 36036195. 18: Vanhooteghem O. Remarkable efficiency of surgical shave excision of keloids followed by intralesional injection of Bleomycin. A retrospective study of 314 cases. Dermatol Ther. 2022 May;35(5):e15425. doi: 10.1111/dth.15425. Epub 2022 Mar 13. PMID: 35261136; PMCID: PMC9285601. 19: Zhao Y, Yan Z, Liu Y, Zhang Y, Shi J, Li J, Ji F. Effectivity of mesenchymal stem cells for bleomycin-induced pulmonary fibrosis: a systematic review and implication for clinical application. Stem Cell Res Ther. 2021 Aug 23;12(1):470. doi: 10.1186/s13287-021-02551-y. PMID: 34420515; PMCID: PMC8380478. 20: Hendel K, Jemec GBE, Haedersdal M, Wiegell SR. Electrochemotherapy with bleomycin for basal cell carcinomas: a systematic review. J Eur Acad Dermatol Venereol. 2021 Nov;35(11):2208-2215. doi: 10.1111/jdv.17492. Epub 2021 Jul 21. PMID: 34219303.