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货号:A159794 同义名: Campathecin;CPT Ambeed 开学季,买赠积分,赢豪礼

Camptothecin (CPT) 是一种生物碱,作为 DNA 拓扑异构酶 I (Topo I) 抑制剂,IC50 为 679 nM。它对结直肠癌、乳腺癌、肺癌和卵巢癌表现出强效的抗肿瘤活性,并通过改变人类癌细胞中的微小 RNA (miRNA) 表达模式来调节缺氧诱导因子 1α (HIF-1α) 活性。

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Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Camptothecin 化学结构 CAS号:7689-03-4
Camptothecin 化学结构
CAS号:7689-03-4
Camptothecin 3D分子结构
CAS号:7689-03-4
Camptothecin 化学结构 CAS号:7689-03-4
Camptothecin 3D分子结构 CAS号:7689-03-4
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Camptothecin 纯度/质量文件 产品仅供科研

货号:A159794 标准纯度: 98%
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 99%+
β-Lapachone 99%+
(s)-10-hydroxycamptothecin 99%+
Camptothecin ++

Topo I, IC50: 0.68 μM

98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

99%+
Topotecan ++++

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

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

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

Topo II, IC50: 15 μM

99%+
Levofloxacin 99%+
Etoposide 98%
Pefloxacin mesylate dihydrate 99+%
Marbofloxacin 99%+
Voreloxin HCl 98%
Mitoxantrone dihydrochloride PKC 99%+
Nalidixic acid 99%+
Doxorubicin 98%
Novobiocin sodium 98%+
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 99%+
Clinafloxacin 97%
Gatifloxacin 99%+
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。

Camptothecin 生物活性

靶点
  • Topo I

    Topo I, IC50:0.68 μM

描述 Camptothecin (CPT), an alkaloid, acts as an inhibitor for DNA topoisomerase I (Topo I) with an IC50 value of 679 nM[1]. Demonstrating significant antitumor effects on colorectal, breast, lung, and ovarian cancers, CPT also affects the activity of hypoxia-inducible factor-1α (HIF-1α) by altering the patterns of microRNAs (miRNA) expression in human cancer cells[2].[3].
体内研究

Administering Camptothecin (2 mg/kg every other day) to mice presenting extensive pulmonary metastases resulted in a significant reduction of these metastases when combined with the kinase inhibitor of nuclear factor-kappaB-1 (KINK-1)[5].

体外研究

MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) cells, characterized by elevated TOP1 enzyme activity, are particularly susceptible to Camptothecin treatment (ranging from 0.1 μM to 5 μM over 72 hours), showing IC50 values of 0.089 μM and 0.067 μM, respectively[4].

A dosage of Camptothecin at 0.5 μM for 6 and 24 hours notably decreases the expression of VEGF activated by desferrioxamine. Furthermore, Camptothecin administration (0.5 μM; 8 to 24 hours) effectively inhibits the accumulation of HIF-1α induced by desferrioxamine[2].

Camptothecin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780 cytotoxicity assay IC50=4 nM 11858737
A427 ~1 μM Growth inhibitory assay IC50=24 nM 9876111
A549 cytotoxicity assay IC50=67 nM 10841808
A549 cytotoxicity assay IC50=14 nM 11334569

Camptothecin 动物研究

Dose Rat: 30 mg/kg[3] (i.g.)
Administration i.g.
Pharmacokinetics
Animal Rats[3]
Dose 30 mg/kg
Administration p.o.
F 1
T1/2 1.843 ± 0.394 h
Tmax 0.500 ± 0.000 h
Cmax 0.656 ± 0.055 nmol/mL
AUC0→∞ 2.749 ± 0.329 nmol/ml·h
AUC0→t 2.694 ± 0.312 nmol/ml·h

Camptothecin 参考文献

[1]Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.

[2]Bertozzi D, et al. The natural inhibitor of DNA topoisomerase I, camptothecin, modulates HIF-1α activity by changing miR expression patterns in human cancer cells. Mol Cancer Ther. 2014;13(1):239-248.

[3]Huang Q, et al. Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. Eur J Med Chem. 2013;63:746-757.

[4]Tesauro C, et al. Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study. BMC Cancer. 2019;19(1):1158. Published 2019 Nov 29.

[5]Schön M, et al. KINK-1, a novel small-molecule inhibitor of IKKbeta, and the susceptibility of melanoma cells to antitumoral treatment. J Natl Cancer Inst. 2008;100(12):862-875..

Camptothecin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.71mL

5.74mL

2.87mL

Camptothecin 技术信息

CAS号7689-03-4
分子式C20H16N2O4
分子量 348.352
别名 Campathecin;CPT;(+)-Camptothecin;20(S)-Camptothecine;d-Camptothecin;Camptothecine;NSC 94600;MAG-CPT;(S)-(+)-Camptothecin
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 5 mg/mL(14.35 mM),配合低频超声助溶,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

1M NaOH: 10 mg/mL(28.71 mM),配合低频超声,并调节pH至11

动物实验配方
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