ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer.
性状
Solid
IC50 & Target[1][2]
FP
790 nM (Ki)
TP Receptor
2400 nM (Ki)
EP4
1.3 nM (Ki)
EP3
30 nM (Ki)
体外研究(In Vitro)
ONO-AE3-208 surpresses the 体外研究 cell invasion and migration in a dose-dependent manner without affecting cell proliferation. ONO-AE3-208 abolisheS CTGF in the presence of the EET synthesis inhibitor MS-PPOH. Arachidonic acid (AA) causeS dose-dependent dilation of the attached Af-Art, and this effect is blocked by ONO-AE3-208.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ONO-AE3-208 surpresses the in vivo bone metastasis of PC3 cells in mice. The photon tumor burdens are significantly increased in a time-dependent manner in the control group in comparison with those in the ONO-AE3-208-treated group. The rate of metastasis formation is significantly higher in the former than in the latter. The median time of metastasis formation is 29 d in the ONO-AE3-208-treated animals as compared with 21 d in the controls.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.