| Identification | Back Directory | [Name]
(8S,10S)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-10-[5-hydroxy-4-[(2S)-2-methoxymorpholin-4-yl]-6-methyl-oxan-2-yl]oxy-1-methoxy-9,10-dihydro-7H-tetracene-5,12-dione | [CAS]
108943-08-4 | [Synonyms]
Nemorubicin HCL
(8S,10S)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-10-[5-hydroxy-4-[(2S)-2-methoxymorpholin-4-yl]-6-methyl-oxan-2-yl]oxy-1-methoxy-9,10-dihydro-7H-tetracene-5,12-dione | [Molecular Formula]
C32H37NO13 | [MOL File]
108943-08-4.mol | [Molecular Weight]
680.1 |
| Hazard Information | Back Directory | [Uses]
Nemorubicin hydrochloride is a derivative of doxorubicin, and has antitumor activity. Nemorubicin hydrochloride, not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. | [in vivo]
Nemorubicin is converted to PNU-159682 by human liver cytochrome P450 (CYP) 3A4 in rat, mouse, and dog liver microsomes[2]. Nemorubicin (60 μg/kg) induces sifnificant tumor growth delay in scid mice bearing 9L/3A4 tumors, but shows no obvious effect on the tumor growth delay of 9L tumors in mice by i.v. or intratumoral injection (i.t.). Nemorubicin (40 μg/kg, i.p.) exhibits no antitumor activity and no host toxicity in mice bearing 9L/3A4 tumors[4]. | [References]
[1] Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11(4):1608-17. DOI:10.1158/1078-0432.CCR-04-1845
[2] Quintieri L, et al. In vitro hepatic conversion of the anticancer agent nemorubicin to its active metabolite PNU-159682 in mice, rats and dogs: a comparison with human liver microsomes. Biochem Pharmacol. 2008 Sep 15;76(6):784-95. DOI:10.1016/j.bcp.2008.07.003
[3] Sabatino MA, et al. Down-regulation of the nucleotide excision repair gene XPG as a new mechanism of drug resistance in human and murine cancer cells. Mol Cancer. 2010 Sep 24;9:259. DOI:10.1186/1476-4598-9-259
[4] Lu H, et al. Potentiation of methoxymorpholinyl doxorubicin antitumor activity by P450 3A4 gene transfer. Cancer Gene Ther. 2009 May;16(5):393-404. DOI:10.1038/cgt.2008.93 |
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