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Camptothecin

MCE China：Camptothecin

Brand：MedChemExpress (MCE)

Cat. No.HY-16560

CAS：7689-03-4

Synonyms：Campathecin; (S)-(+)-Camptothecin; CPT

Purity：99.86%

Storage：4°C, protect from light *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.

In Vitro：High TOP1 enzymatic activity MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) show high sensitivity toward Camptothecin (0.1 μM to 5 μM; 72 hours) treatment, exhibiting the IC50 values of 0.089 μM and 0.067 μM, respectively[4]. Camptothecin (0.5 μM; 6 and 24 hours) reduces desferrioxamine-activated VEGF expression. Camptothecin (0.5 μM; 8 to 24 hours) strongly prevents the desferrioxamine-dependent HIF-1a accumulation[2].

In Vivo：Camptothecin (2 mg/kg every other day) treats mice, has developed numerous pulmonary metastases. Treatment with both kinase inhibitor of nuclear factor-kappaB-1 (KINK-1) and Camptothecin led to a statistically significant reduction in the number of pulmonary metastases[5].

IC50 & Target：Topoisomerase I 679 nM (IC50) Camptothecins

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References：

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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..  [Content Brief]