MF-766 is a highly potent, selective, and orally active EP4 antagonist with a Ki of 0.23 nM, acting as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. It is useful for cancer and inflammation diseases research [1][2].

EP4:0.23 nM (Ki)

MF-766, at concentrations ranging from 0.01 to 10 μM and pretreated for 1 hour before being stimulated with 50 ng/mL IL-2—both with and without 0.33 μM PGE2 for 18 hours—effectively reverses the suppression of IFN-γ secretion in human NK cells caused by PGE2. Importantly, the viability of NK cells remains unaffected by MF-766[2].

MF-766 (oral gavage; 30 mg/kg; once daily; 21 days) exhibits TGI% of 49% in CT26 tumor model. But it does not exhibits significant difference in EMT6 and 4T1 tumor model[2].
MF-766 (oral gavage; 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8) shows potent anti-tumor activities in different preclinical models. The % of TGI are 89%, 66% and 40%, respectively in CT26 tumor, EMT6 and 4T1 tumor model[2].