Etoposide 

Antitumor agent that complexes with topoisomerase II and DNA to enhance double-strand and single-strand cleavage of DNA and reversibly inhibit religation. Blocks the cell cycle in in S-phase and G2-phase of the cell cycle; induces apoptosis in normal and tumor cell lines; inhibits synthesis of the oncoprotein Mdm2 and induces apoptosis in tumor lines that overexpress Mdm2.

synthetic

≥98%

powder

white

9.8

236-251 °C(lit.)

DMSO: 30 mg/mL

human ... ABCB1(5243), CYP3A4(1576), TOP2A(7153)

mouse ... Abcb1a(18671), Abcb1b(18669)

rat ... Top2a(360243)

Hande, K.R., Etoposide: four decades of development of a topoisomerase II inhibitor. Eur. J. Cancer 34, 1514-1521, (1998)

Droin, N., et al., Upregulation of CASP genes in human tumor cells undergoing etoposide-induced apoptosis. Oncogene 16, 2885-2894, (1998)

Arriola, E.L., et al., Differential regulation of p21^waf-1/cip-1 and Mdm2 by etoposide: etoposide inhibits the p53-Mdm2 autoregulatory feedback loop. Oncogene 18, 1081-1091, (1999)

Kaufmann, S.H., Cell death induced by topoisomerase-targeted drugs: more questions than answers. Biochim. Biophys. Acta 1400, 195-211, (1998)

Inaba, M., et al., Different modes of cell-killing action between DNA topoisomerase I and II inhibitors revealed by kinetic analysis. Jpn. J. Cancer Res. 85, 187-193, (1994)

Burden, D.A., et al., Topoisomerase II-etoposide interactions direct the formation of drug-induced enzyme-DNA cleavage complexes. J. Biol. Chem. 271, 29238-29244, (1996)

Sehested, M., and Jensen, P.B., Mapping of DNA topoisomerase II poisons and catalytic inhibitors to four distinct steps in the topoisomerase II catalytic cycle. Biochem. Pharmacol. 51, 879-886, (1996)

Chow, K.C., and Ross, W.E., Topoisomerase-specific drug sensitivity in relation to cell cycle progression. Mol. Cell. Biol. 7, 3119-3123, (1987)

3

KC0190000