1059070-10-8
1059070-10-8 structure
- Name: DSR 6434
- Chemical Name: 6-Amino-2-(butylamino)-9-({6-[2-(dimethylamino)ethoxy]-3-pyridinyl}methyl)-7,9-dihydro-8H-purin-8-one
- CAS Number: 1059070-10-8
- Molecular Formula: C19H28N8O2
- Molecular Weight: 400.478
- Catalog: Signaling Pathways Immunology/Inflammation Toll-like Receptor (TLR)
- Create Date: 2018-07-16 04:52:13
- Modify Date: 2024-01-02 17:13:09
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DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect[1][2].
| Name | 6-Amino-2-(butylamino)-9-({6-[2-(dimethylamino)ethoxy]-3-pyridinyl}methyl)-7,9-dihydro-8H-purin-8-one |
|---|---|
| Synonyms |
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- |
| Description | DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect[1][2]. |
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| Related Catalog | |
| Target |
TLR7:7.2 nM (EC50, Human) TLR7:4.6 nM (EC50, Mice) |
| 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[2]. |
| 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)[1]. Animal Model: B6C3F1 mice injected with HM-1 ovarian cancer cells[1] 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). |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C19H28N8O2 |
| Molecular Weight | 400.478 |
| Exact Mass | 400.233521 |
| LogP | 0.23 |
| Index of Refraction | 1.635 |
| Hazard Codes | Xi |
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