MF-766

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MF-766  纯度: 99.73%

MF-766 是一种高效、选择性和口服活性的 EP4 拮抗剂，Ki 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。

MF-766

MF-766 Chemical Structure

CAS No. : 1050656-06-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4740 In-stock
5 mg ￥4500 In-stock
10 mg ￥8000 In-stock
25 mg ￥16500 In-stock
50 mg ￥25500 In-stock
100 mg ￥38000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MF-766 相关产品

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生物活性

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].

IC50 & Target[1]

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[2].

Shanghai Jinpan Biotech Co Ltd 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[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].

Shanghai Jinpan Biotech Co Ltd 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 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.

分子量

478.46

Formula

C27H21F3N2O3
CAS 号

1050656-06-8
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (104.50 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0900 mL 10.4502 mL 20.9004 mL
5 mM 0.4180 mL 2.0900 mL 4.1801 mL
10 mM 0.2090 mL 1.0450 mL 2.0900 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.23 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
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

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