MF-766
规格
| Cas Number | 1050656-06-8 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 50 mg/mL (104.50 mM; Need ultrasonic) |
| 过滤标签 | Prostaglandin Receptor,GPCR/G Protein |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | MF-766 是一种强效、选择性和口服活性 EP4 拮抗剂，其 K i 为 0.23 nM。在功能测试中，MF-766 表现为完全拮抗剂，IC 50 为 1.4 nM（在存在 10% HS 的情况下升至 1.8 nM）。MF-766可用于癌症的拮抗剂研究。 |
| 英文描述 |
MF-766 is a highly potent, selective and orally active EP4 antagonist with a K i of 0.23 nM. MF-766 behaves as a full antagonist with an IC 50 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57BL/6 J strain mice injected subcutaneously with CT26, EMT6, or 4T1 cellsDosage: 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. Form:Solid IC50& Target:EP4 0.23 nM (Ki) |