化合物E7046 TQ0025

Product Introduction
Bioactivity


英文名: E7046

描述: E7046 是一种口服有效的特异性 EP4拮抗剂，IC50值为 13.5 nM，Ki 值为 23.14 nM，具有抗肿瘤活性。

体外活性: Through selective EP4 antagonism, E7046 reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells [1].

体内活性: E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. The blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells [1]. In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significantly better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors [2].

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

溶解度: DMSO : 100 mg/mL (206.87 mM)


关键字: Inhibitor | Prostaglandin Receptor | E7046 | E 7046 | inhibit | E-7046

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相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Anti-Cancer 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