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Pirarubicin 72496-41-4

Product Description

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Molecular Weight:

627.64 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.

Biological Activity

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. 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.


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). 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.


Pirarubicin
reduces the tumor weight to 60% of the control level in M5076 solid
tumor-bearing mice, although doxorubicin has no effect. 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.

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