[CAS NO. 1059070-10-8] DSR-6434
PRODUCTS SPECIFICATIONS [1059070-10-8]
DESCRIPTION [1059070-10-8]
Overview
| MDL | MFCD30182245 |
|---|---|
| Molecular Weight | 400.48 |
| Molecular Formula | C19H28N8O2 |
| SMILES | O=C1N(C2=NC(NCCCC)=NC(N)=C2N1)CC3=CN=C(OCCN(C)C)C=C3 |
Summary
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 [1] [2] .
IC50 & Target
|
TLR7 7.2 nM (EC 50 , Human) |
TLR7 4.6 nM (EC 50 , 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 624.25 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4970 mL | 12.4850 mL | 24.9700 mL |
| 5 mM | 0.4994 mL | 2.4970 mL | 4.9940 mL |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4970 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1 mg/mL (2.50 mM); Clear solution
References
- [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.