JTE-013 是一种选择性S1P2拮抗剂。它抑制放射性标记的 S1P 与人和大鼠 S1P2的特异性结合，IC50分别为 17 nM 和 22 nM。

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.

383150-41-2

C17H19Cl2N7O

408.29

DMSO:100 mg/mL (244.92 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years