货号:A1193404
同义名:
AB928; A2aR/A2bR antagonist-1
Etrumadenant是一种双重 A2aR/A2bR 拮抗剂,与 A2aR ,A2bR 的平衡结合常数分别为 1.4 nM 和 2 nM。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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 |
98% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 描述 | Adenosine is an endogenous modulator that triggers multiple signaling pathways through four G-protein-coupled adenosine receptors A1R, A2aR, A2bR, and A3R. A2aR and A2bR are the receptors that primarily expressly in immune cells (T cells and myeloid cells, respectively). AB928 is a dual A2aR/A2bR antagonist that inhibits A2aR and A2bR with an equilibrium binding constant of 1.4 and 2 nM, respectively[1]. In the presence of adenosine, human monocyte-derived dendritic cells differentiated and exhibited a reduced ability to stimulate IFN-γ secretion from allogenic CD4+ T-cells in a mixed lymphocyte reaction. However, the addition of AB928 reversed adenosine-mediated suppression of dendritic cell function. AB928 also rescued gene expressions regulated by adenosine during the differentiation of human monocyte-derived dendritic cells[2]. In human whole blood, AB928 at 90 nM inhibited 50% of the 5 μM 5'-N-Ethylcarboxamidoadenosine-induced phosphorylation of cAMP response element-binding protein[3]. In C57BL/6 mice inoculated with mouse mammary tumor AT3-OVA, the concurrent treatment with AB928 and chemotherapy resulted in a significant reduction in tumor volume as compared to chemotherapy alone (28 mg vs. 86 mg). Also, mice treated with both AB928 and chemotherapy exhibited increased immune cell infiltrate and stromal response in tumors. Treatment with AB928 in combination with α-PD-1 therapy also suppressed the growth of melanoma B16-F10 tumors in inoculated mice[2]. |
| Concentration | Treated Time | Description | References | |
| CHO-A2aR cells | 10 µM | 30 minutes | To evaluate the selectivity of DZD2269 for A2aR and its ability to inhibit cAMP accumulation. Results showed DZD2269 effectively inhibited cAMP accumulation stimulated by 10 µM NECA. | J Exp Clin Cancer Res. 2022 Oct 14;41(1):302 |
| SUIT-2-MSLN | 10 nM to 1 μM | 24 hours | Assess the effect of AB928 on human anti-MSLN CAR T cells, demonstrating AB928 restored IFN-γ and IL-2 secretion inhibited by NECA. | Br J Cancer. 2022 Dec;127(12):2175-2185 |
| 4T1, LL/2-EpCAM, T110299-EpCAM, CT26-EpCAM | 100 nM | 24 hours | Validate the protective effect of AB928 on CAR T cell function across different cancer cell lines, showing AB928 reversed NECA-mediated suppression in all cell lines. | Br J Cancer. 2022 Dec;127(12):2175-2185 |
| Panc02-EpCAM | 100 nM to 10 μM | 24 hours | Evaluate the impact of AB928 on CAR T cell cytokine secretion, finding that AB928 fully restored IFN-γ, IL-2, and TNF-α secretion inhibited by NECA. | Br J Cancer. 2022 Dec;127(12):2175-2185 |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c mice | Colon carcinoma model | Oral | 10 mg | Once daily until the end of the experiment | Evaluate the effect of oral AB928 on CAR T cell activation, showing AB928 enhanced CAR T cell activation and promoted an effector-like phenotype. | Br J Cancer. 2022 Dec;127(12):2175-2185 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.72mL 2.34mL 1.17mL |
23.45mL 4.69mL 2.34mL |
|
| CAS号 | 2239273-34-6 |
| 分子式 | C23H22N8O |
| 分子量 | 426.47 |
| SMILES Code | N#CC1=CC=CC(C2=NC(N)=NC(C3=CN(CC4=NC(C(C)(O)C)=CC=C4)N=N3)=C2)=C1C |
| MDL No. | N/A |
| 别名 | AB928; A2aR/A2bR antagonist-1 |
| 运输 | 蓝冰 |
| InChI Key | BUXIAWLTBSXYSW-UHFFFAOYSA-N |
| Pubchem ID | 135242184 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的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
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