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Formula | C32H37NO12 |
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Molecular Weight | 627.64 | CAS No. | 72496-41-4 | |
Solubility (25°C)* | In vitro | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. | |
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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] |
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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] |
Nkx2.8 promotes chemosensitivity in bladder urothelial carcinoma via transcriptional repression of MDR1 [ Cell Death Dis, 2022, 13(5):492] | PubMed: 35610207 |
Lipoparticles for Synergistic Chemo-Photodynamic Therapy to Ovarian Carcinoma Cells: In vitro and in vivo Assessments [ Int J Nanomedicine, 2021, 16:951-976] | PubMed: 33603362 |
Synthesis and In Vitro Assessment of pH-Sensitive Human Serum Albumin Conjugates of Pirarubicin [ Pharmaceuticals (Basel), 2020, 14(1)E22] | PubMed: 33396604 |
Gene Essentiality Profiling Reveals Gene Networks and Synthetic Lethal Interactions with Oncogenic Ras. [ Cell, 2019, 36(2):179-193] | PubMed: 28162770 |
A Pharmacogenomic Landscape in Human Liver Cancers. [ Cancer Cell, 2019, 36(2):179-193] | PubMed: 31378681 |
Dual Inhibition of Pirarubicin-Induced AKT and ERK Activations by Phenformin Sensitively Suppresses Bladder Cancer Growth. [ Front Pharmacol, 2019, 10:1159] | PubMed: 31649535 |
MARCH1 encourages tumour progression of hepatocellular carcinoma via regulation of PI3K-AKT-β-catenin pathways. [ J Cell Mol Med, 2019, 23(5):3386-3401] | PubMed: 30793486 |
Down-regulation of PKM2 enhances anticancer efficiency of THP on bladder cancer [ J Cell Mol Med, 2018, 22(5):2774-2790] | PubMed: 29512924 |
RIPK1 Inhibition Enhances Pirarubicin Cytotoxic Efficacy through AKT-P21-dependent Pathway in Hepatocellular Carcinoma. [ Int J Med Sci, 2018, 15(14):1648-1657] | PubMed: 30588188 |
[ Oncotarget, 2017, ] | PubMed: 29190892 |
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