Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]-
![Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]- Structure](CAS/20210111/GIF/1050656-06-8.gif)
- CAS No.
- 1050656-06-8
- Chemical Name:
- Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]-
- Synonyms
- MF-766;MF-766, 10 mM in DMSO;4-(1-(1-(4-(trifluoromethyl)benzyl)-1H-indole-7-carboxamido)cyclopropyl)benzoic acid;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
- CBNumber:
- CB08246411
- Molecular Formula:
- C27H21F3N2O3
- Molecular Weight:
- 478.46
- MDL Number:
- MOL File:
- 1050656-06-8.mol
Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]- Properties
| 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 |
| FDA UNII | 86KF5VSV88 |
Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]- Chemical Properties,Uses,Production
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)
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
Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
Benzoic acid, 4-[1-[[[1-[[4-(trifluoromethyl)phenyl]methyl]-1H-indol-7-yl]carbonyl]amino]cyclopropyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43340 | 58 |
| Nanjing Chemlin Chemical Co., Ltd | 025-83697070 13913916777 | info@chemlin.com.cn | China | 19244 | 64 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 71826 | 60 |
| Shanghai Chaolan Chemical Technology Center | 021-QQ：65489617 15618227136 | Sales@ATKchemical.com | China | 9342 | 58 |
| Shanghai Dongyang Biotechnology Co., Ltd. | 0512-0512-13601744364 13601744364 | chemsharker@126.com | China | 947 | 58 |
| DC Chemicals | 021-58447131 13564518121 | doncunbiosci@gmail.com | China | 512 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62072 | 58 |
