Home DNA Damage/DNA Repair Antineoplastic and Immunosuppressive Antibiotics inhibitor - Topoisomerase inhibitor Pirarubicin For research use only.

Pirarubicin

Synonyms: NSC-333054,THP

Pirarubicin is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent.

Pirarubicin Chemical Structure

Pirarubicin Chemical Structure

CAS No. 72496-41-4

Purity & Quality Control

Pirarubicin Related Products

Biological Activity

Description Pirarubicin is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent.
Targets
Topo II [1]
In vitro
In vitro

Pirarubicin is rapidly taken up by M5076 cells and the intracellular concentration of pirarubicin reaches more than 2.5-fold that of doxorubicin. Pirarubicin is more effective than doxorubicin in terms of the 50% cell growth-inhibitory concentration in vitro. [1] Pirarubicin causes G0/G1 cell cycle arrest in MG-63 cells. Pirarubicin suppresses the expression of PCNA, cyclin D1, cyclin E and Bcl-2, and increases Bax expression in MG-63 cells. [2] Pirarubicin markedly relaxes contractions induced by noradrenaline (0.1 μM) in the aorta with endothelium, but not in that without endothelium. Pirarubicin-induced relaxation is inhibited by methylene blue (5 μM), hydroquinone (100 μM), phenidone (50 μM), haemoglobin (1 μM) and p-bromophenacyl bromide (50 μM), but not by indomethacin (25 μM). [3] Pirarubicin is approximately 2-5 times more potent than Adriamycin in SKUT1B, HEC1A, and BG1 cell lines. Pirarubicin also displays a reverse dose-response pattern of G2 block so that at high dose, cell cycle kinetics would mirror those of untreated controls. [4]
In Vivo
In vivo

Pirarubicin reduces the tumor weight to 60% of the control level in M5076 solid tumor-bearing mice, although doxorubicin has no effect. [1] Pirarubicin and Epirubicin are effective against V x 2 tumor when injected via the hepatic intra-arterial (h.i.a.) route, the activity of Pirarubicin is stronger than that of Epirubicin. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05099341 Recruiting
Depression
Centre Hospitalier Universitaire Dijon
 October 1 2021 Not Applicable
NCT04158817 Completed
Prostate Cancer
Shanghai General Hospital Shanghai Jiao Tong University School of Medicine|NanoMab Technology (UK) Limited
 November 1 2019 Early Phase 1
NCT03716180 Active not recruiting
Breast Cancer
Dana-Farber Cancer Institute|Susan G. Komen Breast Cancer Foundation|Breast Cancer Research Foundation|Terri Brodeur Breast Cancer Foundation
 November 5 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 627.64 Formula

C32H37NO12
CAS No. 72496-41-4 SDF Download Pirarubicin SDF
Smiles CC1C(C(CC(O1)OC2CC(CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)CO)O)N)OC6CCCCO6
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (159.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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