MF-766

Research use only, not for human use.

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.

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.(In Vitro):MF-766 (0.01-10 μM; pretreatment for 1 h and then stimulated with 50 ng/mL IL-2; with and without 0.33 μM PGE2; 18 hours) reverses PGE2-suppressed IFN-γ secretion in human NK cells. Additionally, NK cell viability is not affected by MF-766.(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.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.

——

Animal Model:Female C57BL/6?J strain mice injected subcutaneously with CT26, EMT6, or 4T1 cells Dosage:30 mg/kg combination with anti-PD-1 mDX400 Administration:Oral gavage; 10 mg/kg or 30 mg/kg combination with anti-PD-1 mDX400; once daily; 21 days; q4dx8 Result:Improved anti-tumor activity in the setting of PD-1 blockade in multiple syngeneic models.

——

GPCR/G Protein

Prostaglandin Receptor

FFA1/GPR40

——

——

1050656-06-8

478.46

C27H21F3N2O3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (104.50 mM)

OC(c1ccc(C2(CC2)NC(c2c3n(Cc4ccc(C(F)(F)F)cc4)ccc3ccc2)=O)cc1)=O

——

(-20℃)

With Ice Pack

≥ 2 years