Camptothecin

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Chemical Structure| 7689-03-4 同义名 : Campathecin; CPT; (+)-Camptothecin; 20(S)-Camptothecine; d-Camptothecin; Camptothecine; NSC 94600; MAG-CPT; (S)-(+)-Camptothecin
CAS号 : 7689-03-4
货号 : A159794
分子式 : C20H16N2O4
纯度 : 98%
分子量 : 348.35
MDL号 : MFCD00081076
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -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
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
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
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..