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DSR-6434

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Chemical Structure| 1059070-10-8 同义名 : -
CAS号 : 1059070-10-8
货号 : A846098
分子式 : C19H28N8O2
纯度 : 99%+
分子量 : 400.478
MDL号 : MFCD30182245
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(299.64 mM)，配合低频超声助溶，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：
生物活性
描述 DSR-6434 is a highly potent TLR7 agonist with EC50 value of 7.2nM for activation of hTLR7 in NF-κB SEAP reporter assay. Administration of DSR-6434, i.v., inhibited lung metastasis by 78% at dose of 0.1mg/kg and suppressed lung metastasis completely at dose of 1 mg/kg on HM-1 metastasis model. DSR-6434 at concentration<5μM alone does not affect tumor cell( CT26 or KHT) clonogenic potential or radio sensitivity in vitro. Intravenous administration of 0.1mg/kg DSR-6434 in combination with IR improved survival in syngeneic models of colorectal carcinoma and fibrosarcoma in vivo, which may due to priming an antitumor CD8+ T-cell response.
作用机制 DSR-6434 possesses 8-oxoadenine structure which is a novel structural class IFN inducer.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.49mL

2.50mL

1.25mL

24.97mL

4.99mL

2.50mL
参考文献

[1]Nakamura T, Wada H, 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, Dovedi SJ, 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.