DSR-6434
目录号: PL12315 纯度: ≥98%
CAS No. :1059070-10-8
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中文名称
DSR-6434
中文别名
DSR 6434
英文名称
DSR-6434
英文别名
DSR 6434;6-Amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]-3-pyridinyl]methyl]-7,9-dihydro-8H-purin-8-one;BDBM50425234;6-amino-2-(butylamino)-9-((6-(2-(dimethylamino)ethoxy)pyridin-3-yl)methyl)-7,9-dihydro-8h-purin-8-one;6-Amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]pyridin-3-yl]methyl]-7H-purin-8-one;DSR-6434
Cas No.
1059070-10-8
分子式
C19H28N8O2
分子量
400.48
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
DSR-6434 是一种有效的选择性的 Toll 样受体 7 (TLR7) 激动剂,对人和小鼠 TLR7 的 EC50 分别为 7.2 nM 和 4.6 nM。DSR-6434 具有很强的抗肿瘤作用。
生物活性
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC 50 s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
性状
Solid
IC50 & Target[1][2]
TLR7 7.2 nM (EC50, Human) TLR7 4.6 nM (EC
体外研究(In Vitro)
To assess the specificity of DSR-6434 toward TLR7, an NF-κB-driven reporter assay is performed in HEK293 cells engineered to express either hTLR7, TLR8 or TLR9. In this assay, successful binding of DSR-6434 to the specific receptor leads to NF-κB activation. DSR-6434 is capable of stimulating reporter gene activity only in HEK293 cells expressing hTLR7 and not in HEK293 cells expressing the structurally similar hTLR8 or hTLR9. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
DSR-6434 treatment (Compound 20; 0.1-1 mg/kg; intravenous injection; biweekly; for 4 weeks; B6C3F1 mice) suppresses the lung metastasis significantly, 78% inhibition at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group). 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
参考文献
[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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (624.25 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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