Bleomycin hydrochloride

Name: Bleomycin hydrochloride
Brand: MedChemExpress
SKU: HY-17565A
Rating: 5.0 (103 reviews)

Cat. No.: HY-17565A Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic.

For research use only. We do not sell to patients.

Bleomycin hydrochloride Chemical Structure

CAS No. : 67763-87-5

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Based on 103 publication(s) in Google Scholar

Other Forms of Bleomycin hydrochloride:

Bleomycin sulfate In-stock
Bleomycin Get quote

103 Publications Citing Use of MCE Bleomycin hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic^[1].

In Vitro

Bleomycin hydrochloride is chosen as the best-studied micronucleus inducers in human lymphocytes with different mechanisms of genotoxicity. The most frequent Bleomycin-induced DNA lesions are single and double strand breaks and single apuinic/apyrimidinic sites. At the same time Bleomycin is true radiomimetic compound, resembling almost completely the genetic effect of ionizing radiation^[1].
The IC₅₀ value of Bleomycin hydrochloride for UT-SCC-19A cell line is 4.0±1.3 nM. UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin; IC₅₀ values are 14.2±2.8 nM and 13.0±1.1 nM, respectively^[2].
Bleomycin hydrochloride (50, 100 μM; for 24, 48 h) induce pulmonary fibrosis in RLE-6TN cell (50 μM) and A549 cell (100 μM)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bleomycin sulfate can be used to create animal models of pulmonary fibrosis. Intratracheal administration of Bleomycin sulfate (3.5-4.0 mg/kg) on day 0 elicits a treatment response, characterized by a decrease in body weight of the subjects on day 4, followed by recovery and continued growth until the end of the experiment. This treatment also significantly increases the levels of hydroxyproline in lung tissue and the mass of the right caudal lobe of the lung. In 8-week-old male BALB/c mice (weighing approximately 20-30 grams), intratracheal instillation of Bleomycin sulfate at a dose of 5.0 mg/kg/day induces pulmonary fibrosis and promotes the expression of α-SMA and type I collagen. Similarly, in 8-week-old male C57BL/6 mice (average weight around 24.5 grams), intratracheal injection of 2.5 mg/kg Bleomycin sulfate effectively induces pulmonary fibrosis. Bleomycin sulfate is rapidly absorbed after administration via intramuscular, subcutaneous, intraperitoneal, or intrapleural routes, reaching peak plasma concentrations within approximately 60 minutes. When given intravenously, less than 1% of the drug binds to plasma proteins, ensuring high bioavailability. The mean plasma clearance rate of Bleomycin sulfate is about 70 mL/min/m², indicating high plasma elimination and urinary excretion rates^[3]^[4]^[5]^[6].

Induction of Pulmonary Fibrosis^[7]

Background

Bleomycin sulfate can lead to lung patchy parenchymal inflammation, epithelial cell injury with reactive hyperplasia, epithelial-mesenchymal transition, activation and differentiation of fibroblasts to myofibroblasts, and basement membrane and alveolar epithelium injures. The experimental use of Bleomycin sulfate is to induce pulmonary fibrosis animal models.

Specific Mmodeling Methods

Mice: C57BL/6 • 12-week-old
Administration: 3-5 mg/kg • intratracheal administration • sprays on day one

Note

The mice were housed in separate stainless-steel cages (six mice per cage) in a temperature-controlled environment (20-24°C) on 12 h light-dark cycles with unrestricted access to food and water.

Modeling Indicators

Body quality changes: The appetite activity is reduced, with the fur less shiny, the spirits being lethargic, and the bodyweight decreasing. Showed shortness of breath, coughing, and noisy.
Lung changes: Increased fibrotic consolidations, non-aerated lung area, and high-density lung area. Pulmonary function decreased.
Molecular changes: Increased indicators: TGF-β1, TNF-α, IL-6, and GM-CSF in bronchoalveolar lavage fluid.

Correlated Product(s): Bleomycin hydrochloride (HY-17565A)

Opposite Product(s): Neotuberostemonine (HY-N3196)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Fischer 344 rats, 8-10 week old, weighing 150-250 g^[3]
Dosage:	3.5-4 mg/kg
Administration:	Intra-tracheal
Result:	Body weights decreased by day 4 then increased by Day 7 through the end of the study.

Clinical Trial

CAS No.

67763-87-5

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C)N[C@H](C(N[C@H](C)[C@@H](O)[C@H](C)C(N[C@]([C@H](O)C)([H])C(NCCC2=NC(C3=NC(C(N[R])=O)=CS3)=CS2)=O)=O)=O)[C@H](C4=CN=CN4)O[C@H]5[C@H]([C@H]([C@@H]([C@@H](O5)CO)O)O)O[C@]6([H])[C@H]([C@H]([C@@H]([C@H](O6)CO)O)OC(N)=O)O.NC(NCCCC[R])=N.[R]CCC[S+](C)C.[H]Cl.[R=].[Bleomycin A2].[R=].[Bleomycin B2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (Need ultrasonic)

DMSO : 50 mg/mL (ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL; Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (281 KB) SDS (419 KB)

COA (248 KB) HNMR (428 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Hovhannisyan G, et al. Comparative analysis of individual chromosome involvement in micronuclei induced by bleomycin in human leukocytes. Mol Cytogenet. 2016 Jun 21;9:49. [Content Brief]

[2]. Jaaskela-Saari HA, et al. Squamous cell cancer cell lines: sensitivity to bleomycin and suitability for animal xenograft studies. Acta Otolaryngol Suppl. 1997;529:241-4. [Content Brief]

[3]. Corboz MR, et al. Therapeutic administration of inhaled INS1009, a LRX-15 prodrug formulation, inhibits bleomycin-induced pulmonary fibrosis in rats. Pulm Pharmacol Ther. 2018 Apr;49:95-103. [Content Brief]

[4]. Kang Miao, et al. Scutellarein inhibits BLM-mediated pulmonary fibrosis by affecting fibroblast differentiation, proliferation, and apoptosis. Ther Adv Chronic Dis. 2020 Jul 30;11:2040622320940185. [Content Brief]

[5]. Ling Peng, et al. Scutellarin ameliorates pulmonary fibrosis through inhibiting NF-κB/NLRP3-mediated epithelial-mesenchymal transition and inflammation. Cell Death Dis. 2020 Nov 13;11(11):978. [Content Brief]