吡柔比星 T6628

Product Introduction
Bioactivity


英文名: Pirarubicin

描述: Pirarubicin (Theprubicin) 是一种蒽环类抗生素，是拓扑异构酶 II 抑制剂，可用于各种癌症的研究。

体外活性: 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]

体内活性: Pirarubicin在携带M5076实体瘤的小鼠中，将肿瘤重量降低到对照组的60%，而Doxorubicin却没有效果。[1] 通过肝内动脉(h.i.a.)注射，Pirarubicin和Epirubicin对V x 2肿瘤有效，Pirarubicin的活性强于Epirubicin。[5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 7 mg/mL (11.15 mM)


关键字: Topoisomerase | Bacterial | inhibit | Pirarubicin | Autophagy | Inhibitor | Antibiotic

相关产品: Levofloxacin hydrate | Lupalbigenin | 9-amino-CPT | Topoisomerase II inhibitor 13 | Pazufloxacin Mesylate | Betulinic acid | Ac-Exatecan | Doxorubicin hydrochloride | Oxaquin TEA | Razoxane

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Approved Drug Library | Anti-Breast Cancer Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Target-Focused Phenotypic Screening Library

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