GENZ-644282 - CAS 529488-28-6
Catalog number: 529488-28-6
Category: Inhibitor
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Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
white solid powder
GENZ-644282; GENZ644282; GENZ 644282.
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1.Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment.
Kurtzberg LS1, Roth S, Krumbholz R, Crawford J, Bormann C, Dunham S, Yao M, Rouleau C, Bagley RG, Yu XJ, Wang F, Schmid SM, Lavoie EJ, Teicher BA. Clin Cancer Res. 2011 May 1;17(9):2777-87. doi: 10.1158/1078-0432.CCR-10-0542. Epub 2011 Mar 17.
PURPOSE: Genz-644282 [8,9-dimethoxy-5-(2-N-methylaminoethyl)-2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-one] has emerged as a promising candidate for antitumor agents. This report describes the bone marrow colony-forming unit, granulocyte macrophage (CFU-GM) and tumor cell CFU activity of topoisomerase I (Top1) inhibitors, such as Genz-644282, topotecan, irinotecan/SN-38, and ARC-111, and examines their activity in several human tumor xenograft models.
2.Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program.
Houghton PJ1, Lock R, Carol H, Morton CL, Gorlick R, Anders Kolb E, Keir ST, Reynolds CP, Kang MH, Maris JM, Billups CA, Zhang MX, Madden SL, Teicher BA, Smith MA. Pediatr Blood Cancer. 2012 Feb;58(2):200-9. doi: 10.1002/pbc.23016. Epub 2011 May 5.
BACKGROUND: Genz-644282 is a novel non-camptothecin topoisomerase I poison that is in clinical development.
3.Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282.
Sooryakumar D1, Dexheimer TS, Teicher BA, Pommier Y. Mol Cancer Ther. 2011 Aug;10(8):1490-9. doi: 10.1158/1535-7163.MCT-10-1043. Epub 2011 Jun 2.
Camptothecin derivatives are powerful anticancer drugs because of their ability to trap topoisomerase I (Top1)-DNA cleavage complexes. However, they exhibit clinical limitations due to the instability of their α-hydroxylactone six-membered E-ring structure. In addition, they exhibit bone marrow and intestinal toxicity, especially in adults, and are drug efflux substrates. Here, we report a novel Top1 inhibitor, Genz-644282. We show that Genz-644282 and its metabolites induce Top1 cleavage at similar, as well as unique genomic positions, compared with camptothecin. The compound also induces protein-linked DNA breaks and Top1-DNA cleavage complexes that persist longer after compound removal than camptothecin. Concentration-dependent and persistent γH2AX formation was readily observed in cells treated with Genz-644282, and was present in greater than 50% of the cell population following 24 hours compound exposure. The compound shows partial cross-resistance in cell lines resistant to camptothecin.
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