Camptothecin

貨號 Cat. No.: C-330
規格 Size: 10 x 10 mg 250mg 5x250mg

Description

Camptothecin

Topoisomerase Inhibitor

Product#:

C-330

Sizes:

10 x 10 mg

250 mg

5 x 250 mg

M.W.:

348.36

CAS No.:

[7689-03-4]

Structure:

Purity:

>99%

Bioassay:

Campotothecin inhibits the proliferation of MCF-7 breast cancer cells.

MCF-7 cells were treated with different concentrations of Campotothecin (#C-330) for four days;

the number of live cells was measured by XTT cell proliferation assay kit,

normalized to the control (100%) and plotted against drug concentration.

References:

1.	Hsiang, Y.H. et al. (1985) J. Biol. Chem. 260, 14873.
2.	Capranico, G. et al. (1990) Nucleic Acids Res. 18, 6611.
3.	Chen, A. Y., and Liu, L. F. (1994) Annu. Rev. Pharmacol. Toxicol. 34, 191.
4.	Tanizawa, A. et al. (1993) J. Biol. Chem. 268, 25463.
5.	Wang, J. C. (1996) Annu. Rev. Biochem. 65, 635.
6.	Kaufmann, S. H. (1998) Biochim. Biophys. Acta 1400, 195.
7.	Pommier, Y. et al. (1998) Biochim. Biophys. Acta 1400, 83.
8.	Jaxel, C. et al. (1991) J. Biol. Chem. 266, 20418.
9.	Li, C.J. et al. (1994) J. Biol. Chem. 269, 7051.
10.	Shao, R.G. et al. (1997) J. Biol. Chem. 272, 31321

Camptothecin is an anti-cancer alkaloid that specifically inhibits DNA topoisomerase I and DNA topoisomerase II (topoisomerase I/II).^1-3 The highly conserved region around Gly505 of the topoisomerase I was found to be important for camptothecin activity.⁴

Camptothecin converts topoisomerase into a cell poison by trapping the cleavable covalent complex of enzyme with duplex DNA and blocking the re-ligation step. Thereby enhancing and stabilizing the formation of DNA breakage which is responsible for cell death.^1-9

Camptothecin inhibits (IC₅₀ = 30 nM) Tat protein-mediated transactivation of HIV-1 and enhances PKCa activity during apoptosis in HL60 myeloid leukemia cells via a caspase-regulated mechanism.^9,10

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