| Description | DSR-6434 is a selective agonist of TLR7 with antitumor effect. DSR-6434 exhibits EC50s of 7.2 nM and 4.6 nM for human and mouse. |
| In vitro | 为评估DSR-6434对TLR7的特异性，采用了NF-κB驱动的报告基因检测方法在转基因HEK293细胞中进行，这些细胞分别表达hTLR7、TLR8或TLR9。在此检测中，DSR-6434与特定受体的成功结合会激活NF-κB。实验结果显示，DSR-6434仅能在表达hTLR7的HEK293细胞中刺激报告基因活性，而在表达结构相似的hTLR8或hTLR9的HEK293细胞中则无此能力[1]。 |
| In vivo | 在B6C3F1小鼠中，DSR-6434（0.1-1 mg/kg；静脉注射）显著抑制了肺转移[1]。 |
| Target activity | TLR7:4.6 nM (EC50, Mice), TLR7:7.2 nM (EC50, Human) |
| molecular weight | 400.48 |
| Molecular formula | C19H28N8O2 |
| CAS | 1059070-10-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 225 mg/mL (561.8 mM), Sonication is recommended. |
| References | 1. Nakamura T, et al. Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility. Bioorg Med Chem Lett. 2013 Feb 1;23(3):669-72. 2. Adlard AL, et al. A novel systemically administered Toll-like receptor 7 agonist potentiates the effect of ionizing radiation in murine solid tumor models. Int J Cancer. 2014 Aug 15;135(4):820-9. |