Banoxantrone dihydrochloride (AQ4N dihydrochloride) (Synonyms: AQ4N dihydrochloride) |
| Catalog No.GC34085 |
Le dihydrochlorure de banoxantrone (dihydrochlorure d'AQ4N) est un nouvel agent bioreducteur qui peut être réduit en un composé stable et affinitaire pour l'ADN, AQ4, qui est un puissant inhibiteur de la topoisomérase II.
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Cas No.: 252979-56-9
Sample solution is provided at 25 µL, 10mM.
Banoxantrone dihydrochloride (AQ4N dihydrochloride) is an oxygen-depleted activated topoisomerase II inhibitor, AQ4N binds to DNA in a non-covalent manner and promotes antitumor activity of hypoxic and hypoxic tumor cells[1-4].
AQ4N(0-0.25 mM;24h) showed 8-fold higher cytotoxicity under hypoxia than normoxia in cultures of 9L rat gliosarcoma and H460 human non-small-cell lung carcinoma cells[5].
AQ4N(200 mg/kg; i.p.; 30 minutes before radiation) was combined with radiation, considerable DNA damage was detected in T50/80 tumors implanted in BDF mice after immediate excision[2,6].Activation of AQ4N cytotoxicity in mice requires extensive and prolonged tumor hypoxia[5]. AQ4N inhibited HMEC-1 cell contacts on Matrigel, HMEC-1 cell invasion, and sprouting in rat aorta explants. When AQ4N (20 mg/kg) was given in vivo for 5 days, microvessels disappeared in LNCaP tumors grown in a dorsal skin flap[7].
References:
[1]. Newell DR, Searle KM, Westwood NB, Burtles SS; Cancer Research UK Phase I/II Clinical Trials Committee. Professor Tom Connors and the development of novel cancer therapies by the Phase I/II Clinical Trials Committee of Cancer Research UK. Br J Cancer. 2003 Aug 4;89(3):437-54. doi: 10.1038/sj.bjc.6601106. PMID: 12888809; PMCID: PMC2394365.
[2]. Hejmadi MV, McKeown SR, et,al. DNA damage following combination of radiation with the bioreductive drug AQ4N: possible selective toxicity to oxic and hypoxic tumour cells. Br J Cancer. 1996 Feb;73(4):499-505. doi: 10.1038/bjc.1996.87. PMID: 8595165; PMCID: PMC2074454.
[3]. Patterson LH, McKeown SR, et,al. Enhancement of chemotherapy and radiotherapy of murine tumours by AQ4N, a bioreductively activated anti-tumour agent. Br J Cancer. 2000 Jun;82(12):1984-90. doi: 10.1054/bjoc.2000.1163. PMID: 10864207; PMCID: PMC2363261.
[4]. Patterson LH, McKeown SR. AQ4N: a new approach to hypoxia-activated cancer chemotherapy. Br J Cancer. 2000 Dec;83(12):1589-93. doi: 10.1054/bjoc.2000.1564. PMID: 11104551; PMCID: PMC2363465.
[5]. Manley E Jr, Waxman DJ. Impact of tumor blood flow modulation on tumor sensitivity to the bioreductive drug banoxantrone. J Pharmacol Exp Ther. 2013 Feb;344(2):368-77. doi: 10.1124/jpet.112.200089. Epub 2012 Nov 28. PMID: 23192656; PMCID: PMC3558827.
[6]. McKeown SR, Hejmadi MV, et,al. AQ4N: an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo. Br J Cancer. 1995 Jul;72(1):76-81. doi: 10.1038/bjc.1995.280. PMID: 7599069; PMCID: PMC2034137.
[7]. O'Rourke M, Ward C, et,al. Evaluation of the antiangiogenic potential of AQ4N. Clin Cancer Res. 2008 Mar 1;14(5):1502-9. doi: 10.1158/1078-0432.CCR-07-1262. PMID: 18316575.
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