Camptothecin

Source: isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native in China.

Active Product:

Appearance: yellow powder

Brand name(s):
Chemical Name: 4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-(4H,12H)-dione
Molecular Weight: M.W. 348.352
Solubility:  Poorly soluble in water (< 1 mg/ml) and ethanol, soluble in DMSO (5 mg/ml). Also soluble in chloroform/methanol (4:1): 4 mg/mL. Aliquot and store at -20 °C
Storage: 2-8°C

Target: topoisomerase I inhibitor.  Approximately 0.5 µM CPT induces 50% topo I DNA cleavage (Holden et al, 1999)

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Comment

As a topoisomerase I inhibitor, (S)-(+)-Camptothecin binds irreversibly to the DNA-topoisomerase I complex, inhibiting the reassociation of DNA after cleavage by topoisomerase I and traps the enzyme in a covalent linkage with DNA. The enzyme complex is ubiquinated and destroyed by the 26S proteasome, thus depleting cellular topoisomerase I.

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Synonym:  CPT

Molecular Formula: C₂₀H₁₆N₂O₄

- Lerchen HG. Camptothecin antitumor agents. IDrugs. 1999 Sep;2(9):896-906.

- Holden JA, Wall ME, Wani MC, Manikumar G. Human DNA topoisomerase I: quantitative analysis of the effects of camptothecin analogs and the benzophenanthridine alkaloids nitidine and 6-ethoxydihydronitidine on DNA topoisomerase I-induced DNA strand breakage. Arch Biochem Biophys. 1999 Oct 1;370(1):66-76.

- Wall ME, Wani MC.Camptothecin. Discovery to clinic. Ann N Y Acad Sci. 1996 Dec 13;803:1-12.