Camptothecin

Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. 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[2][3].

Product Specifications

CAS Number

[7689-03-4]

Product Name Alternative

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

UNSPSC

12352005

Hazard Statement

H301, H340

Target

ADC Payload; Antibiotic; Apoptosis; Fungal; Influenza Virus; MicroRNA; Topoisomerase

Type

Natural Products

Related Pathways

Antibody-drug Conjugate/ADC Related; Anti-infection; Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/Campathecin.html

Purity

99.86

Solubility

1M NaOH : 10 mg/mL (ultrasonic; adjust pH to 11 with NaOH) |DMSO : 6.25 mg/mL (ultrasonic)

Smiles

O=C1C2=C([C@@](O)(CC)C(OC2)=O)C=C(N1C3)C(C3=C4)=NC5=C4C=CC=C5

Molecular Formula

C20H16N2O4

Molecular Weight

348.36

Precautions

H301, H340

References & Citations

[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]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..|[4]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.|[5]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.