化合物MF-766 T9622

Product Introduction
Bioactivity


英文名: MF-766

描述: MF-766 是高效的、具有口服活性的EP4选择性拮抗剂，Ki 为 0.23 nM。它在功能检测中表现为一种完整的拮抗剂，其 IC50为 1.4 nM (在 10% HS 存在时变成 1.8 nM)。它具有用于癌症和炎症疾病研究的价值。

体外活性: MF-766（0.01-10μM；预处理1小时后再以50ng/mL IL-2刺激；同时考虑是否存在0.33μM PGE2；18小时）能够逆转PGE2对人NK细胞中IFN-γ分泌的抑制作用。此外，MF-766[2]对NK细胞的存活率无影响。

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (104.50 mM)


关键字: EP4 | arthritis | inflammation disease | AIA | inhibit | MF-766 | anti-tumor | MF766 | MF 766 | Prostaglandin Receptor | Inhibitor | cancer

相关产品: mPGES1-IN-3 | CAY10678 | Sucralfate | Pizuglanstat | Eupatolide | EP1-antagonist-1 | Ralinepag | Chamigrenal | ONO-8713 | 3-O-Acetyl-α-boswellic acid

相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Orally Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途