MF-766

CAS No. 1050656-06-8

MF-766( —— )

Catalog No. M28808 CAS No. 1050656-06-8

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.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    MF-766
  • Note
    Research use only, not for human use.
  • Brief 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.
  • 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.(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.
  • In Vitro
    ——
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Prostaglandin Receptor
  • Recptor
    FFA1/GPR40
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1050656-06-8
  • Formula Weight
    478.46
  • Molecular Formula
    C27H21F3N2O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (104.50 mM)
  • SMILES
    OC(c1ccc(C2(CC2)NC(c2c3n(Cc4ccc(C(F)(F)F)cc4)ccc3ccc2)=O)cc1)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes J. Med. Chem., 2008, 51 (22), pp 7061-7064
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