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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 腺苷受体 / Imaradenant

Imaradenant 99%+

货号：A592542 同义名： AZD4635;HTL1071 Ambeed 开学季，买赠积分，赢豪礼

AZD4635 is an A2AR antagonist which can reverse adenosine mediated T cell suppression.

Imaradenant 化学结构 CAS号：1321514-06-0
Imaradenant 化学结构
CAS号：1321514-06-0
Imaradenant 3D分子结构
CAS号：1321514-06-0
Imaradenant 化学结构 CAS号：1321514-06-0
Imaradenant 3D分子结构 CAS号：1321514-06-0
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Imaradenant 纯度/质量文件 产品仅供科研

货号：A592542 标准纯度： 99%+
批次查询： 批次纯度:

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产品名称 Adenosine Receptor ↓ 其他靶点 纯度
ZM241385 ✔ 99%+
Istradefylline +++

Adenosine A2A receptor, Ki: 2.2 nM

 		99%+
Reversine +

human A3 adenosine receptor, Ki: 0.66 μM

 		98%
SCH58261 ++++

bovine A2a, Ki: 2.0 nM

rat A2a, Ki: 2.3 nM

 		99%+
A2A receptor antagonist 1 ++

A1R, Ki: 264 nM

A2AR, Ki: 4 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Imaradenant 生物活性

描述 AZD4635 is an oral A2AR antagonist with Ki value of 1.7nM for affinity to human A2AR, > 30-fold selectivity over other adenosine receptors. AZD4635 inhibited cAMP production in CHO cells stably expressing human A2AR with IC50 values of 0.79, 10.0 and 142.9 nM in the presence of 0.1, 1 and 10 μM adenosine, respectively. AZD4635 reversed suppression and restored IFNγ secretion in cells incubated NECA, a stable analog of adenosine, in an ex vivo CD8+ T cell assay. AZD4635 led to a reduction in tumor growth alone and in combination with checkpoint inhibitors, and enhanced antitumor immunity as tumors harvested from the treated mice exhibited changes in infiltrating lymphocyte populations and increases in the functional activity of T cells.

Imaradenant 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03381274 Carcinoma, Non-Small-Cell Lung Phase 1 Phase 2 Recruiting December 29, 2021 United States, California ... 展开 >> Research Site Recruiting La Jolla, California, United States, 92093 Research Site Recruiting San Francisco, California, United States, 94143 Research Site Withdrawn Santa Monica, California, United States, 90404 United States, Colorado Research Site Recruiting Aurora, Colorado, United States, 80045 United States, Connecticut Research Site Recruiting New Haven, Connecticut, United States, 06510 United States, Florida Research Site Not yet recruiting Gainesville, Florida, United States, 32608 United States, Georgia Research Site Recruiting Atlanta, Georgia, United States, 30322 United States, Illinois Research Site Not yet recruiting Chicago, Illinois, United States, 60611 United States, Maryland Research Site Recruiting Baltimore, Maryland, United States, 21224 United States, New York Research Site Recruiting New York, New York, United States, 10032 United States, Texas Research Site Recruiting Houston, Texas, United States, 77030 Korea, Republic of Research Site Recruiting Seoul, Korea, Republic of, 03080 Research Site Recruiting Seoul, Korea, Republic of, 06351 Research Site Recruiting Seoul, Korea, Republic of, 138-736 Taiwan Research Site Not yet recruiting Taichung, Taiwan, 40705 Research Site Not yet recruiting Taipei City, Taiwan, 10050 收起 <<
NCT03710434 Healthy Volunteers Phase 1 Recruiting April 4, 2019 United Kingdom ... 展开 >> Research Site Recruiting Ruddington, United Kingdom, NG11 6JS 收起 <<
NCT02740985 Advanced Solid Malignancies ... 展开 >> Non-Small Cell Lung Cancer (NSCLC) Metastatic Castrate-Resistant Prostate Carcinoma (mCRPC) Colorectal Carcinoma (CRC) 收起 << Phase 1 Recruiting May 13, 2020 United States, California ... 展开 >> Research Site Recruiting Fresno, California, United States, 93720 United States, Colorado Research Site Recruiting Denver, Colorado, United States, 80218 United States, Connecticut Research Site Not yet recruiting New Haven, Connecticut, United States, 06519 United States, Florida Research Site Not yet recruiting Daytona Beach, Florida, United States, 32117 Research Site Not yet recruiting Lecanto, Florida, United States, 34461 Research Site Not yet recruiting North Port, Florida, United States, 34288 Research Site Recruiting Sarasota, Florida, United States, 34232 United States, Illinois Research Site Recruiting Decatur, Illinois, United States, 62526 United States, Massachusetts Research Site Not yet recruiting Boston, Massachusetts, United States, 02215 United States, Nebraska Research Site Not yet recruiting Omaha, Nebraska, United States, 68130 United States, Nevada Research Site Recruiting Las Vegas, Nevada, United States, 89119 United States, New York Research Site Recruiting New York, New York, United States, 10032 United States, North Carolina Research Site Recruiting Durham, North Carolina, United States, 27710 United States, Pennsylvania Research Site Recruiting Philadelphia, Pennsylvania, United States, 19107 United States, South Carolina Research Site Not yet recruiting Myrtle Beach, South Carolina, United States, 29572 United States, Tennessee Research Site Not yet recruiting Chattanooga, Tennessee, United States, 37404 Research Site Recruiting Nashville, Tennessee, United States, 37203 收起 <<

Imaradenant 参考文献

[1]Preclinical pharmacodynamics and antitumor activity of AZD4635, a novel adenosine 2A receptor inhibitor that reverses adenosine mediated T cell suppression

Imaradenant 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.84mL

3.17mL

1.58mL

31.67mL

6.33mL

3.17mL

Imaradenant 技术信息

CAS号1321514-06-0
分子式C15H11ClFN5
分子量 315.733
别名 AZD4635;HTL1071
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 85 mg/mL(269.22 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Imaradenant | AZD4635;HTL1071 | Adenosine Receptor | AmBeed-信号通路专用抑制剂 | Imaradenant 纯度/质量文件 | Imaradenant 亚型比较 | Imaradenant 生物活性 | Imaradenant 临床数据 | Imaradenant 参考文献 | Imaradenant 实验方案 | Imaradenant 技术信息

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