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1059070-10-8

中文名稱 DSR 6434
英文名稱 DSR 6434
CAS 1059070-10-8
分子式 C19H28N8O2
分子量 400.48
MOL 文件 1059070-10-8.mol
更新日期 2025/01/14 09:41:24
1059070-10-8 結(jié)構(gòu)式 1059070-10-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11108
化合物DSR-6434
6-氨基-2-(丁氨基)-9-((6-(2-(二甲氨基)乙氧基)吡啶-3-基)甲基)-7,9-二氫-8H-嘌呤-8-酮
英文別名
DSR 6434
6-Amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]-3-pyridinyl]methyl]-7,9-dihydro-8H-purin-8-one
8H-Purin-8-one, 6-amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]-3-pyridinyl]methyl]-7,9-dihydro-

物理化學(xué)性質(zhì)

密度1.283±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO:145.03(Max Conc. mg/mL);362.12(Max Conc. mM)
酸度系數(shù)(pKa)10.22±0.20(Predicted)
形態(tài)固體
顏色Light yellow to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H315-H319-H335
防范說(shuō)明P261-P305+P351+P338
DSR 6434價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/02/08HY-110120DSR-64341059070-10-81 mg495元
2025/02/08HY-110120DSR 6434
DSR-6434
1059070-10-85mg1300元
2025/02/08HY-110120DSR 6434
DSR-6434
1059070-10-810mM * 1mLin DMSO1430元

常見問題列表

生物活性
DSR-6434 是一種有效的選擇性的 Toll 樣受體 7 (TLR7) 激動(dòng)劑,對(duì)人和小鼠 TLR7 的 EC50 分別為 7.2 nM 和 4.6 nM。DSR-6434 具有很強(qiáng)的抗腫瘤作用。
靶點(diǎn)

TLR7

7.2 nM (EC 50 , Human)

TLR7

4.6 nM (EC 50 , Mice)

體外研究

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.

體內(nèi)研究

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).

Animal Model: B6C3F1 mice injected with HM-1 ovarian cancer cells
Dosage: 0.1 mg/kg, 1 mg/kg
Administration: Intravenous injection; biweekly; for 4 weeks
Result: Suppressed the lung metastasis significantly, 78% inhibition was seen at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group).
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