MF-766|cas:1050656-06-8|西域试剂

MF-766,99.73%

产品编号：Bellancom-115487| CAS NO：1050656-06-8| 分子式：C₂₇H₂₁F₃N₂O₃| 分子量：478.46

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货号	价格	库存与货期
Bellancom-115487	￥3400.00	杭州北京（现货）
Bellancom-115487	￥5500.00	杭州北京（现货）
Bellancom-115487	￥11000.00	杭州北京（现货）

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MF-766

产品介绍

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 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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。