1059070-10-8
1059070-10-8 結(jié)構(gòu)式
基本信息
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
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)
常見問題列表
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TLR7 7.2 nM (EC 50 , Human) |
TLR7 4.6 nM (EC 50 , Mice) |
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.
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). |