| Identification | Back Directory | [Name]
Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]- | [CAS]
1050656-06-8 | [Synonyms]
MF-766
Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]-
EP4,arthritis,inflammation disease,AIA,inhibit,anti-tumor,MF766,MF 766,MF-766,Prostaglandin Receptor,Inhibitor,cancer | [Molecular Formula]
C27H21F3N2O3 | [MOL File]
1050656-06-8.mol | [Molecular Weight]
478.46 |
| Chemical Properties | Back Directory | [Boiling point ]
711.4±60.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
4.35±0.10(Predicted) | [color ]
Off-white to gray |
| Hazard Information | Back Directory | [Uses]
MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 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. MF-766 can be used for cancer and inflammation diseases research[1][2]. | [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]. | Animal Model: | Female C57BL/6?J strain mice injected subcutaneously with CT26, EMT6, or 4T1 cells[2] | | 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. |
| [IC 50]
EP4: 0.23 nM (Ki) | [storage]
Store at -20°C | [References]
[1] John Colucci, et al. Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain. Bioorg Med Chem Lett DOI:10.1016/j.bmcl.2010.04.065
[2] Yun Wang, et al. Combination of EP 4 antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both DOI:10.1080/2162402X.2021.1896643 |
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DC Chemicals
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021-58447131 13564518121 |
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www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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