Evixapodlin|2374856-75-2|(GS-4224; PD-1/PD-L1-IN 7)-陌孚医药/Medlife

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Evixapodlin (Synonyms: GS-4224; PD-1/PD-L1-IN 7)

目录号: PL08985 纯度: ≥98%

CAS No. :2374856-75-2

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中文名称	Evixapodlin
英文名称	Evixapodlin
英文别名	(5S,5'S)-5,5'-((((5,5'-(2,2'-dichloro-[1,1'-biphenyl]-3,3'-diyl)bis(3-methoxypyrazine-5,2-diyl))bis(methylene))bis(azanediyl))bis(methylene))bis(pyrrolidin-2-one);PD-1/PD-L1-IN 7;2-Pyrrolidinone, 5,5'-[(2,2'-dichloro[1,1'-biphenyl]-3,3'-diyl)bis[(3-methoxy-5,2-pyrazinediyl)methyleneiminomethylene]]bis-, (5S,5'S)-;evixapodlin;LJ1WH7GQ72;Evixapodlin [INN];BDBM451999;US10710986, Example 139;Evixapodlin
Cas No.	2374856-75-2
分子式	C₃₄H₃₆Cl₂N₈O₄
分子量	691.61
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Evixapodlin (GS-4224) 是一种人 PD-1/PD-L1 蛋白/蛋白相互作用的抑制剂，IC₅₀ 为 0.213 nM。Evixapodlin 具有抗癌和抗病毒功能。

生物活性

Evixapodlin (GS-4224) is a human PD-1/PD-L1 protein/protein interaction inhibitor with an IC 50 of 0.213 nM. Evixapodlin has anticancer and antiviral functions.

性状

Solid

IC50 & Target[1][2]

IC50: 0.213 nM (Human PD-1/PD-L1 protein/protein interaction)

体外研究(In Vitro)

Evixapodlin (compound 139) enhances IFN-γ and Granzyme B Production in chronic hepatitis B (CHB) CD8 T Cells and CD4 T Cells. Evixapodlin also enhances the frequency of GrB cells among HBV-specific CD8 and CD4 T cells. The ability of Evixapodlin to enhance the antiviral functions of HBV-specific CD8 and CD4 T cells in vitro is comparable to those of Durvalumab. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Evixapodlin (Compound 139; 10-50 mg/kg; intraperitoneal injection, daily, for 6 days) treatment shows >90% PD-L1 target occupancy (TO) on the tumor cells. Evixapodlin significantly inhibits tumor growth in a human PD-L1 expressing MC38 mouse colorectal 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

ClinicalTrial

参考文献

[1]. Evangelos Aktoudianakis, et al. Pd-1/pd-l1 inhibitors. WO2019160882A1.