Voreloxin Hydrochloride

• CAT Number: I002288
• CAS Number: 175519-16-1
• Molecular Formula: C18H20ClN5O4S
• Molecular Weight: 437.9
• Purity: ≥95%
• Target: Topoisomerase
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C

Voreloxin Hcl(SNS-595; AG 7352) is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II.IC50 Value:Target: Topoisomerase IIVosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication. As a result, inhibition of DNA replication, RNA and protein synthesis occurs, followed by cell cycle arrest at G2 phase and induced p53-independent apoptosis. This agent shows a favorable toxicity profile in several aspects: it does not generate reactive oxygen species, as do anthracyclines, reducing the risk of cardiotoxicity; it is not a P-glycoprotein (P-gp) substrate, and thereby evades the common mechanism for multidrug resistance; and it has limited distribution to normal tissues and a more chemically stable molecular structure.

Reference

[1]. Hoch U, Lynch J, Sato Y et al. Voreloxin, formerly SNS-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models. Cancer Chemother Pharmacol. 2009 Jun;64(1):53-65.
[2]. Hawtin RE, Stockett DE, Byl JA et al. Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. PLoS One. 2010 Apr 15;5(4):e10186.
[3]. Lancet JE, Ravandi F, Ricklis RM et al. A phase Ib study of vosaroxin, an anticancer quinolone derivative, in patients with relapsed or refractory acute leukemia. Leukemia. 2011 Dec;25(12):1808-14.
[4]. Krug LM, Crawford J, Ettinger DS et al. Phase II multicenter trial of voreloxin as second-line therapy in chemotherapy-sensitive or refractory small cell lung cancer. J Thorac Oncol. 2011 Feb;6(2):384-6.
[5]. Advani RH, Hurwitz HI, Gordon MS et al. Voreloxin, a first-in-class anticancer quinolone derivative, in relapsed/refractory solid tumors: a report on two dosing schedules. Clin Cancer Res. 2010 Apr 1;16(7):2167-75.
[6]. Study of Vosaroxin or Placebo in Combination With Cytarabine in Patients With First Relapsed or Refractory Acute Myeloid Leukemia (AML)