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| Product | Description | |
|---|---|---|
| Elomotecan | Elomotecan (BN-80927) belongs to a novel family of camptothecin analogs, the homocamptothecins, developed on the concept of topoisomerase I (Topo I) inhibition and characterized by a stable seven-membered beta-hydroxylactone ring. Preclinical data reported here show that BN80927 retains Topo I poisoning activity in cell-free assay (DNA relaxation) as well as in living cells, in which in vivo complexes of topoisomerase experiments and quantification of DNA-protein-complexes stabilization, have confirmed the higher potency of BN80927 as compared with the Topo I inhibitor SN38. In addition, BN80927 inhibits Topo II-mediated DNA relaxation in vitro but without cleavable-complex stabilizatio...th assays, BN80927 is a very potent antiproliferative agent as shown by IC(50) values consistently lower than those of SN38 in tumor cell lines as well as in their related drug-resistant lines. BN80927 shows high efficiency in vivo in tumor xenograft studies using human androgen-independent prostate tumors PC3 and DU145. Altogether, these data strongly support the clinical development of BN80927. Synonyms: BN-80927; BN80927; BN 80927; R-1559; R1559; R 1559; (R)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-((4-methylpiperidin-1-yl)methyl)-4, 5-dihydrooxepino[3', 4':6, 7]indolizino[1, 2-b]quinoline-3, 15(1H, 13H)-dione. CAS No. 220998-10-7. Molecular formula: C29H32ClN3O4. Mole weight: 522.04. |  |
| Elomotecan HCl salt | Elomotecan, also referred to BN 80927 and R 1559, characterized by a stable seven-membered beta-hydroxylactone ring, is a DNA topoisomerase inhibitor. In vivo elomotecan shows high efficiency in vivo in tumor xenograft studies using human androgen-independent prostate tumors PC3 and DU145. Synonyms: 220997-99-9; 220998-10-7 (Elomotecan free base); (5R)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-[(4-methylpiperidin-1-yl)methyl]-1,4,5,13-tetrahydro-3H,15H-oxepino[3',4':6,7]indolizino[1,2-b]quinoline-3,15-dione hydrochloride (1:1). Grades: >98%. CAS No. 220997-99-9. Molecular formula: C29H33Cl2N3O4. Mole weight: 558.5. | |
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