MF-766

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MF-766 是一种高效、选择性、口服活性的 EP4 拮抗剂，Ki 为 0.23 nM。在功能测定中，它作为完全拮抗剂，IC50 为 1.4 nM（在 10% HS 存在下，IC50 变为 1.8 nM）。它可用于癌症和炎症疾病的研究。

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.

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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.

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GPCR/G Protein

Prostaglandin Receptor

FFA1/GPR40

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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

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(-20℃)

With Ice Pack

≥ 2 years