| Description | MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. It behaves 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 can be used for cancer and inflammation diseases research[1][2]. |
| In vitro | MF-766（0.01-10μM；预处理1小时后再以50ng/mL IL-2刺激；同时考虑是否存在0.33μM PGE2；18小时）能够逆转PGE2对人NK细胞中IFN-γ分泌的抑制作用。此外，MF-766[2]对NK细胞的存活率无影响。 |
| In vivo | 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]. |
| Target activity | EP4:0.23 nM (Ki) |
| molecular weight | 478.46 |
| Molecular formula | C27H21F3N2O3 |
| CAS | 1050656-06-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (125.4 mM), Sonication is recommended. |