EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.target: HIF1αIC 50:20-40 nM.[1]in vitro : EL102 is a cytotoxic agent and also displays cytostatic properties, through flow cytometric analysis of PI-stained cells cultured for 24, 48 and 72?h, following treatment. EL102 induces apoptosis and causes G2/M arrest, preventing the cell from entering into mitosis.In vivo: CWR22 tumours were taken from an in vivo passage, cut into small fragments and transplanted subcutaneously (s.c.) into the flank of 48 nude mice. At day 13, when the tumours were palpable, mice were randomised into 10 groups with 8 mice each and treatment initiated. EL102 12mg?kg?1 via p.o. (0700 hours and 1700 hours daily).[1]
[1]. A P Toner et al. The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivoactivity against prostate cancer and circumvents MDR1 resistance. Br J Cancer, 2013 Oct 15, 109(8): 2131-2141.