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Ethonafide

NMR下載 COA and HPLC MSDS下載
names：
2-(2'-(dimethylamino)ethyl)-1,2-dihydro-7-ethoxydibenz(de, h)isoquinoline-1,3-dione
CAS號：
175293-23-9
MDL Number：
MF(分子式)： C22H22N2O3 MW(分子量)： 362.42
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	Ethonafide
英文別名	AMP53
CAS號	175293-23-9
Inchi	InChI=1S/C22H22N2O3/c1-4-27-20-15-9-6-5-8-14(15)19-18-16(20)10-7-11-17(18)21(25)24(22(19)26)13-12-23(2)3/h5-11H,4,12-13H2,1-3H3
InchiKey	CQZISUJEDPJJNF-UHFFFAOYSA-N
分子式 Formula	C22H22N2O3
分子量 Molecular Weight	362.42
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	Ethonafide(CAS:175293-23-9):僅限應(yīng)用于工業(yè)或者科學(xué)研究過程中非醫(yī)療目的，不應(yīng)用于人類或動物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerated and more effective at inhibiting tumor growth compared with mitoxantrone in a human xenograft tumor regression mouse model. Mechanistically, we found that ethonafide inhibited topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIalpha and -beta. In addition, ethonafide induced a potent G(2) cell cycle arrest in the DU 145 human prostate cancer cell line. By creating stable cell lines with decreased expression of topoisomerase IIalpha or -beta, we found that a decrease in topoisomerase IIalpha protein expression renders the cell line resistant to ethonafide. The decrease in sensitivity to ethonafide was associated with a decrease in DNA damage and an increase in DNA repair as measured by the neutral comet assay. These data demonstrate that ethonafide is a topoisomerase II poison and that it is topoisomerase IIalpha-specific in the DU 145 human prostate cancer cell line. (See http//www.ncbi.nlm.nih.gov/pubmed/17351106.)
Application1
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Application3

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[1]Congdon LM, Pourpak A, Escalante AM, Dorr RT, Landowski TH. Proteasomal inhibition stabilizes topoisomerase IIalpha protein and reverses resistance to the topoisomerase II poison ethonafide (AMP-53, 6-ethoxyazonafide). Biochem Pharmacol. 2008 Feb 15;75(4):883-90. Epub 2007 Nov 4. PubMed PMID: 18062937; PubMed Central PMCID: PMC2271051.

[2]Piao WH, Wong R, Bai XF, Huang J, Campagnolo DI, Dorr RT, Vollmer TL, Shi FD. Therapeutic effect of anthracene-based anticancer agent ethonafide in an animal model of multiple sclerosis. J Immunol. 2007 Dec 1;179(11):7415-23. PubMed PMID: 18025185.

[3] Pourpak A, Landowski TH, Dorr RT. Ethonafide-induced cytotoxicity is mediated by topoisomerase II inhibition in prostate cancer cells. J Pharmacol Exp Ther. 2007 Jun;321(3):1109-17. Epub 2007 Mar 9. PubMed PMID: 17351106.

[4] Dorr RT, Liddil JD, Sami SM, Remers W, Hersh EM, Alberts DS. Preclinical antitumor activity of the azonafide series of anthracene-based DNA intercalators. Anticancer Drugs. 2001 Mar;12(3):213-20. PubMed PMID: 11290869.

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