MF-766|1050656-06-8|-陌孚医药/Medlife

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MF-766

目录号: PL10113 纯度: ≥99%

CAS No. :1050656-06-8

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中文名称	MF-766
英文名称	MF-766
英文别名	86KF5VSV88;4-(1-(1-(4-(trifluoromethyl)benzyl)-1H-indole-7-carboxamido)cyclopropyl)benzoic acid;BDBM50319837;Benzoic acid, 4-(1-(((1-((4-(trifluoromethyl)phenyl)methyl)-1H-indol-7-yl)carbonyl)amino)cyclopropyl)-;Q27269749;4-[1-[[1-[[4-(trifluoromethyl)phenyl]methyl]indole-7-carbonyl]amino]cyclopropyl]benzoic acid;4-{1-[({1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl}carbonyl)amino]cyclopropyl}benzoic Acid;MF-766
Cas No.	1050656-06-8
分子式	C₂₇H₂₁F₃N₂O₃
分子量	478.46
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	MF-766 是一种高效、选择性和口服活性的 EP4 拮抗剂，K_i 值为 0.23 nM。MF-766 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)。MF-766 可用于癌症和炎症疾病研究。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	EP4 0.23 nM (Ki)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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 [2]. Yun Wang, et al. Combination of EP 4 antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both

溶解度数据	In Vitro: DMSO : 50 mg/mL (104.50 mM; Need ultrasonic)配制储备液

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