RH1 (NSC 697726) is a potent bioreductive agent with profound anti-cancer activity in vitro and in vivo.
Treatment of NQ16 cells with RH1 (50 and 100 nM) for 60 and 120 min results in a significant increase (p< 0.05) in cross-linked DNA. RH1 induces apoptosis in a time- and concentration-dependent manner in NQ16 cells [1].
RH1 exhibits antitumor activity in a dose-dependent manner against NQ16 tumors growing in athymic mice. RH1 treatment (0.4 mg/kg and 0.2 mg/kg) of mice bearing NQ16 tumors results in a significant reduction in tumor volume between treated groups and controls as early as 5 days after the treatment period ended. Low-dose RH1 (0.1 mg/kg) also results in a significant reduction in tumor volume between treated mice and controls[2].
[1]. Park MT, et al. The anti-tumour compound, RH1, causes mitochondria-mediated apoptosis by activating c-Jun N-terminal kinase. Br J Pharmacol. 2011 Jun;163(3):567-85. [2]. Dehn DL, et al. Development of a new isogenic cell-xenograft system for evaluation of NAD(P)H:quinone oxidoreductase-directed antitumor quinones: evaluation of the activity of RH1. Clin Cancer Res. 2004 May 1;10(9):3147-55.