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> Bleomycin (sulfate) [9041-93-4]

Bleomycin (sulfate) [9041-93-4]

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Referentie HY-17565-10mg

Formaat : 10mg

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

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Bleomycin sulfate Chemical Structure

Bleomycin sulfate Chemical Structure

CAS No. : 9041-93-4

This product is a controlled substance and not for sale in your territory.

Based on 81 publication(s) in Google Scholar

Other Forms of Bleomycin sulfate:

  • Bleomycin hydrochloride In-stock
  • Bleomycin Obtenir un devis

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Description

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

IC50 & Target

DNA/RNA Synthesis[1]
In Vitro

Bleomycin (BLM) sulfate is chosen as the best-studied micronucleus (MN) 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 sulfate 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 (BLM); IC50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively[2].
Bleomycin sulfate (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.

Bleomycin sulfate Related Antibodies
In Vivo

Bleomycin (BLM) sulfate is chosen as the best-studied micronucleus (MN) 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 sulfate 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 (BLM); IC50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively[2].
Bleomycin sulfate (50, 100 μM; for 24, 48 h) induce pulmonary fibrosis in RLE-6TN cell (50 μM) and A549 cell (100 μM)[4].

Bleomycin suLfate (3.5-4.0 mg/kg; intratracheal instillation) significantly increased lung hydroxyproline levels and increased right caudal lobe mass; body weight decreased on day 4 and then increased on day 7[3].
Bleomycin suLfate (5.0 mg/kg/d; intratracheal instillation) induces pulmonary fibrosis and increases α-SMA and collagen I in BALB/c mice (20-30 g; 8 weeks old; male) The expression level[4].
Bleomycin sulfate (2.5 mg/kg; 1.25 mg/mL, 50 μL; intratracheal instillation) induces pulmonary fibrosis in male C57BL/6 mice (8 weeks old, approximately 24.5 g)[5].
Bleomycin sulfate is quickly absorbed following intramuscular, subcutaneous, intraperitoneal, or intrapleural administration and reaches peak plasma concentrations in approximately 60 min. Less than 1% of the drug given intravenously binds to plasma proteins, leading to high bioavailability. Additionally, a mean plasma drug clearance approaching 70 mL/min/m2 has been calculated for Bleomycin sulfate. Bleomycin sulfate possesses a high plasma elimination rate and high urinary excretion rate[6].
Bleomycin sulfate can be used to construct model of pulmonary fibrosis.

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 Modeling 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.
Essai clinique
Masse moléculaire

1523 (average)

CAS No.

9041-93-4
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)(17)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(17)[C@H]([C@H]([C@@H]([C@H](O6)CO)O)OC(N)=O)O.NC(NCCCC[R])=N.[R]CCC[S+](C)C.O=S(O)(O)=O.[R=].[Bleomycin A2].[R=].[Bleomycin B2]
Structure Classification
  • Antibiotics
  • Disease Research
  • Anticancer
  • Antibiotics
  • Other Antibiotics
  • Antibiotics
  • Mammalian Cell Culture
  • Antibiotics
  • Resistance Selection
Initial Source
  • Microorganisms

Streptomyces verticillus
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

H2O : 255 mg/mL (Need ultrasonic and warming)

DMSO : 41.67 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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 (Infinity mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • Protocol 2

    Add each solvent one by one:  Saline

    Solubility: 100 mg/mL (Infinity mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
Pureté et documentation

Purity: 99.49%

COA (309 KB) HNMR (246 KB) LCMS (98 KB)

Instruction de manipulation (2659 KB)
Références

  • [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 treprostinil prodrug formulation, inhibits bleomycin-induced pulmonary fibrosis in rats. Pulm Pharmacol Ther. 2018 Apr;49:95-103.  [Content Brief]

    [4]. 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]

    [5]. 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]

    [6]. Brandt JP, et, al. Bleomycin. National Library of Medicine. August 28, 202

    [7]. Gul A, et, al. Pulmonary fibrosis model of mice induced by different administration methods of bleomycin. BMC Pulm Med. 2023 Mar 21;23(1):91.  [Content Brief]

  • [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.

    [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.

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

    [4]. 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.

    [5]. 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.

    [6]. Brandt JP, et, al. Bleomycin. National Library of Medicine. August 28, 202

    [7]. Gul A, et, al. Pulmonary fibrosis model of mice induced by different administration methods of bleomycin. BMC Pulm Med. 2023 Mar 21;23(1):91.

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Bleomycin sulfate Related Classifications

  • Induced Disease Models Products
  • Respiratory System Disease Models
  • Cell Cycle/DNA Damage Anti-infection
  • DNA/RNA Synthesis Antibiotic
Help & FAQs

Keywords:

Bleomycin9041-93-4DNA/RNA SynthesisAntibioticInhibitorinhibitorinhibit

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