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/ 拓扑异构酶 / Pirarubicin/吡柔比星

Pirarubicin/吡柔比星 {[allProObj[0].p_purity_real_show]}

货号：A154529 同义名： THP; NSC-333054

Pirarubicin是一种蒽环类抗生素，通过抑制拓扑异构酶 II 来发挥抗肿瘤作用，适用于各种癌症的研究。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Pirarubicin/吡柔比星 化学结构 CAS号：72496-41-4
Pirarubicin/吡柔比星 化学结构
CAS号：72496-41-4
Pirarubicin/吡柔比星 3D分子结构
CAS号：72496-41-4
Pirarubicin/吡柔比星 化学结构 CAS号：72496-41-4
Pirarubicin/吡柔比星 3D分子结构 CAS号：72496-41-4
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Pirarubicin/吡柔比星 纯度/质量文件 产品仅供科研

货号：A154529 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Topo I ↓ Topo II ↓ Topo IV ↓ Topoisomerase ↓ 其他靶点 纯度
Ellagic acid ✔ 98%
β-Lapachone ✔ 99%+
(s)-10-hydroxycamptothecin ✔ 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

 		98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

 		98%
Topotecan ++++

Topo I (DU-145 Luc cells), IC50: 2 nM

Topo I (MCF-7 Luc cells), IC50: 13 nM

 		98%
Irinotecan HCl Trihydrate ✔ 98%
SN-38 ✔ 98%
Levofloxacin hydrate ✔ 98%
Dexrazoxane ✔ 99%+
Ofloxacin ✔ 98+%
Enoxacin ✔ 99%+
Flumequine +

Topo II, IC50: 15 μM

 		98%
Levofloxacin ✔ 97%
Etoposide ✔ 98%
Pefloxacin mesylate dihydrate ✔ 99.5%
Marbofloxacin ✔ 98+%
Voreloxin HCl ✔ 98%
Mitoxantrone 2HCl ✔ PKC 98%
Nalidixic acid ✔ 98%
Doxorubicin ✔ 97%
Novobiocin sodium ✔ 95%
Amonafide ✔ 99%+
Pirarubicin ✔ 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

 		99%+
Genistein ✔ EGFR 98%
Teniposide ✔ 98%
Moxifloxacin ✔ 98%
Ciprofloxacin ✔ 98%
Clinafloxacin ✔ 99%
Gatifloxacin ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Epirubicin HCl ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Pirarubicin/吡柔比星 生物活性

靶点

  • Topo II
描述 Pirarubicin is a cell cycle nonspecific anthracycline anticancer drug[3]. It interacts with topoisomerase II to inhibit DNA replication. Pirarubicin inhibits the growth of human HeLa and C33A cervical, as well as T-24 bladder cancer cells (IC50s = 29, 52, and 36 ng/ml, respectively)[4]. It inhibits the growth of human Huh7 and MHCC97H liver cancer cells (IC50s = 0.159 and 0.374 μM, respectively)[5]. Pirarubicin also inhibits the growth of M5076 mouse ovarian cancer cells in vitro (IC50 = 0.366 μM) and in vivo in a mouse allograft model when administered at a dose of 2 mg/kg for four days[6].

Pirarubicin/吡柔比星 细胞实验

Cell Line
Concentration Treated Time Description References
MDA-MB-468 3 μM 24 h To study the effect of THP on circZCCHC2 expression in MDA-MB-468 cells, the results showed that THP significantly downregulated circZCCHC2 expression. iScience. 2024 Jan 26;27(3):109057.
MDA-MB-231 5 μM 24 h To study the effect of THP on circZCCHC2 expression in MDA-MB-231 cells, the results showed that THP significantly downregulated circZCCHC2 expression. iScience. 2024 Jan 26;27(3):109057.
MDA-MB-231 cells 20 μg/mL 2 h To evaluate the cellular uptake and drug release of P60-ICG-THP triggered by acidic pH, the results showed that THP could immediately cross the cell membrane and enter the nucleus at pH 6.5, while ICG was mainly located in the cytoplasm. Theranostics. 2020 Oct 27;10(26):12158-12173.
HCM cells 5 μM 24 h To evaluate the effect of Pirarubicin on the survival rate of HCM cells, the results showed that 5 μM Pirarubicin treatment for 24 h significantly reduced cell viability. Front Pharmacol. 2024 Mar 18;15:1315001.
H9c2 cells 5 μM 24 h To evaluate the effect of Pirarubicin on the survival rate of H9c2 cells, the results showed that 5 μM Pirarubicin treatment for 24 h significantly reduced cell viability. Front Pharmacol. 2024 Mar 18;15:1315001.
H9C2 cardiomyocytes 5 μM 22 h Establish THP-induced cell injury model, THP significantly decreased cell activity Front Pharmacol. 2021 Oct 15;12:733805.

Pirarubicin/吡柔比星 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Xenograft tumor model Tail vein injection 5 mg/kg Once a week for four weeks To study the effect of circZCCHC2 on THP sensitivity in vivo, the results showed that circZCCHC2 overexpression partially rescued the tumor inhibitory effect of THP. iScience. 2024 Jan 26;27(3):109057.
Nude mice MDA-MB-231 tumor model Caudal vein injection 20 mg/kg Once daily for 21 days To evaluate the antitumor effect of P60-ICG-THP in vivo, the results showed that P60-ICG-THP significantly inhibited tumor growth through the combination of chemotherapy, photothermal therapy, and starvation therapy. Theranostics. 2020 Oct 27;10(26):12158-12173.
Wistar rats Pirarubicin-induced cardiotoxicity model Caudal vein injection 3 mg/kg Once a week for 6 weeks To evaluate the effect of Pirarubicin on cardiotoxicity in rats, the results showed that Pirarubicin significantly reduced cardiac function and increased serum levels of myocardial enzymes. Front Pharmacol. 2024 Mar 18;15:1315001.
SD rats THP-induced cardiotoxicity model Caudal vein injection 3 mg/kg Once a week for 8 weeks To study THP-induced cardiotoxicity and observe the protective effect of SchB. THP caused decreased and food intake, abnormal ECG and echocardiogram, myocardial tissue damage, and increased cardiomyocyte apoptosis, which were effectively alleviated by SchB Front Pharmacol. 2021 Oct 15;12:733805.

Pirarubicin/吡柔比星 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03277716 Hepatocellular Carcinoma Non-r... 展开 >>esectable Transarterial Chemoembolization Microwave Ablation 收起 << Not Applicable Recruiting December 30, 2021 China, Beijing ... 展开 >> Cancer Institute &Hospital, Chinese Academy of Medical Sciences Not yet recruiting Beijing, Beijing, China, 100021 Contact: Xiao Li, M.D          China, Fujian The First Affiliated Hospital of Fujian Medical University Recruiting Fuzhou, Fujian, China, 350005 Contact: Zhenyu Lin, M.D.          The tumor hospital of Fujian Province Not yet recruiting Fuzhou, Fujian, China, 350014 Contact: Hailan Lin, M.D          China, Guangdong the First Affiliated Hospital of SunYat-senUniversity Not yet recruiting Guangzhou, Guangdong, China, 510080 Contact: Jiaping Li, M.D          Shenzhen People's Hospital Recruiting Shenzhen, Guangdong, China, 518020 Contact: Yanfang Zhang, M.D.          Peking University Hospital of Shenzhen Recruiting Shenzhen, Guangdong, China, 518036 Contact: Junhui Chen, M.D.          China, Shandong The Second Affiliated Hospital of Shandong University Recruiting Jinan, Shandong, China, 250000 Contact: Yuliang Li, M.D          Shandong Province Hospital Recruiting Jinan, Shandong, China, 250014 Contact: Xin Ye, M.D          the Affiliated Hospital of Medical College Qingdao University Recruiting Qingdao, Shandong, China, 26555 Contact: Zixiang Li, M.D          China, Zhejiang The First Affiliated Hospital of Zhejiang University Not yet recruiting Hangzhou, Zhejiang, China, 310003 Contact: Junhui Sun, M.D. 收起 <<
NCT00131053 Lymphoblastic Leukemia, Acute Phase 2 Unknown September 2011 Japan ... 展开 >> Department of Hematology, Nagoya University Graduate School of Medicine Recruiting Nagoya, Japan, 466-8550 Contact: Fumihiko Hayakawa, MD       bun-hy@med.nagoya-u.ac.jp    Principal Investigator: Fumihiko Hayakawa, MD 收起 <<
NCT02760953 Urinary Bladder Neoplasms Not Applicable Not yet recruiting December 31, 2018 -

Pirarubicin/吡柔比星 参考文献

[1]Liu SY, Song SX, et al. Molecular mechanism of cell apoptosis by paclitaxel and pirarubicin in a human osteosarcoma cell line. Chemotherapy. 2010;56(2):101-7.

[2]Sugiyama T, Sadzuka Y, et al. Membrane transport and antitumor activity of pirarubicin, and comparison with those of doxorubicin. Jpn J Cancer Res. 1999 Jul;90(7):775-80.

[3] Huang H, Chen T, Zhou Y, et al. RIPK1 Inhibition Enhances Pirarubicin Cytotoxic Efficacy through AKT-P21-dependent Pathway in Hepatocellular Carcinoma. Int J Med Sci. 2018;15(14):1648-1657.

[4]Tsuchiya KS, Ishii T, Ikeno S, et al. Inhibition of anchorage-independent growth of tumor cells by IT-62-B, a new anthracycline. J Antibiot (Tokyo). 1997;50(10):853-859.

[5]Huang H, Chen T, Zhou Y, Geng L, Shen T, Zhou L, Zheng S. RIPK1 Inhibition Enhances Pirarubicin Cytotoxic Efficacy through AKT-P21-dependent Pathway in Hepatocellular Carcinoma. Int J Med Sci. 2018 Nov 5;15(14):1648-1657.

[6]Sugiyama T, Sadzuka Y, Nagasawa K, Ohnishi N, Yokoyama T, Sonobe T. Membrane transport and antitumor activity of pirarubicin, and comparison with those of doxorubicin. Jpn J Cancer Res. 1999;90(7):775-780.

Pirarubicin/吡柔比星 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.97mL

1.59mL

0.80mL

15.93mL

3.19mL

1.59mL

Pirarubicin/吡柔比星 技术信息

CAS号72496-41-4
分子式C32H37NO12
分子量 627.64
SMILES Code O=C1C2=C(C=CC=C2OC)C(C3=C(O)C4=C([C@@H](O[C@@]5([H])C[C@H](N)[C@H](O[C@@]6([H])OCCCC6)[C@H](C)O5)C[C@@](C(CO)=O)(O)C4)C(O)=C31)=O
MDL No. MFCD00869742
别名 THP; NSC-333054
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 9 mg/mL(14.34 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

Tags: Pirarubicin | 72496-41-4 | THP | Topoisomerase | Autophagy Inducer | Cell Cycle/DNA Damage | Autophagy | Anti-infection | Topoisomerase | Autophagy | Bacterial | Antibiotic | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Pirarubicin/吡柔比星 纯度/质量文件 | Pirarubicin/吡柔比星 亚型比较 | Pirarubicin/吡柔比星 生物活性 | Pirarubicin/吡柔比星 临床数据 | Pirarubicin/吡柔比星 参考文献 | Pirarubicin/吡柔比星 实验方案 | Pirarubicin/吡柔比星 技术信息

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