JTE-013

JTE-013 is an effective and specific antagonist of S1P2. JTE-013 suppresses the specific binding of radiolabeled S1P to human and rat S1P2 (IC50s: 17 nM and 22 nM, respectively) .JTE-013 is a S1P2 antagonist. JTE-013 (50-200 μM; 1-3 days) decreased cell viability. JTE-013 shows 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM. JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation.JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) decreases tumor size and tumor weight. the modification of JTE-013 to produce the AB1 compound improved potency, intravenous pharmacokinetics, cellular activity, and antitumor activity in NB and may have enhanced clinical and experimental applicability.