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Pirarubicin

CAS号

72496-41-4

分子式

C32H37NO12

主要靶点

Antibiotic|Autophagy|Antibacterial|Topoisomerase

仅限科研使用

Cat No : CM06713

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Synonyms

Inhibitor|Pirarubicin|吡柔比星|Topoisomerase|Topo II|THP|Theprubicin|Antibiotic|Bacterial|Autophagy|inhibit

验证数据展示

  • CAS No.: 72496-41-4

    Pirarubicin
    CAS#: 72496-41-4

产品信息

CAS号 72496-41-4
分子式 C32H37NO12
主要靶点 Antibiotic|Autophagy|Antibacterial|Topoisomerase
主要通路 微生物学|DNA 损伤和修复|微生物学|自噬
分子量 627.64
纯度 98.66%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|Pirarubicin|吡柔比星|Topoisomerase|Topo II|THP|Theprubicin|Antibiotic|Bacterial|Autophagy|inhibit

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]

体外活性

Pirarubicin被M5076细胞迅速吸收，其细胞内浓度超过doxorubicin的2.5倍以上。在体外50%细胞生长抑制浓度方面，Pirarubicin比doxorubicin更有效。[1]Pirarubicin在MG-63细胞中引起G0/G1期细胞周期阻滞，并抑制PCNA、cyclin D1、cyclin E和Bcl-2的表达，同时增加MG-63细胞中Bax的表达。[2]Pirarubicin显著抑制由去甲肾上腺素（0.1 μM）引起的内皮存在的大鼠主动脉收缩。Pirarubicin引起的松弛效应被亚甲蓝（5 μM）、对苯二酚（100 μM）、Phenidone（50 μM）、血红蛋白（1 μM）和p-溴苯乙酰溴（50 μM）抑制，而对 indomethacin（25 μM）则无抑制作用。[3]相比于Adriamycin，Pirarubicin在SKUT1B、HEC1A和BG1细胞系中的效力大约高出2-5倍。Pirarubicin还显示出一种逆剂量-反应模式，即在高剂量下，细胞周期动力学将反映未处理对照的情况。[4]

溶解度

Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:6.26 mg/mL (9.98 mM)

参考文献

1.Sugiyama T, et al. Jpn J Cancer Res, 1999, 90(7), 775-780.
2.Liu SY, et al. Chemotherapy, 2010, 56(2), 101-107.
3.Hirano S, et al. J Pharm Pharmacol, 1991, 43(12), 848-854.
4.Nguyen HN, et al. Gynecol Oncol, 1992, 45(2), 164-173.
5.Okada M, et al. Br J Cancer, 1995, 71(3), 518-524.
6.Li K, et al. Pirarubicin induces an autophagic cytoprotective response through suppression of the mammalian target of rapamycin signaling pathway in human bladder cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):380-5.
7.Wang YD, et al. Cardioprotective effects of rutin in rats exposed to pirarubicin toxicity. J Asian Nat Prod Res. 2017 Oct 27:1-13.

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