Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
DSR-6434 (DSR6434) is a novel and selective Toll-like receptor 7 (TLR7) agonist with antitumor effects. It activated TLR7 with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 exhibited an optimal balance between the agonistic potency and high water solubility. It also demonstrated a strong antitumor effect in vivo by intravenous administration in a tumor bearing mice model.
ln Vitro |
An NF-κB-driven reporter experiment is carried out in HEK293 cells that have been modified to express either hTLR7, TLR8, or TLR9 in order to evaluate the selectivity of DSR-6434 toward TLR7. In this experiment, NF-κB is activated upon successful binding of DSR-6434 to the particular receptor. Only HEK293 cells expressing hTLR7 can be stimulated by DSR-6434 to activate reporter genes; HEK293 cells expressing hTLR8 or hTLR9, which are physically identical, cannot be stimulated[2].
|
---|---|
ln Vivo |
Compound 20 (0.1–1 mg/kg; intravenous injection; every two weeks; B6C3F1 mice) administered intraperitoneally for four weeks strongly suppresses lung metastasis, with 78% suppression at 0.1 mg/kg dose (no tumor metastasis in the 1 mg/kg group)[1].
|
Animal Protocol |
Animal/Disease Models: B6C3F1 mice injected with HM-1 ovarian cancer cells[1]
Doses: 0.1 mg/kg, 1 mg/kg Route of Administration: intravenous (iv) injection; biweekly; for 4 weeks Experimental Results: Suppressed the Lung metastasis Dramatically, 78% inhibition was seen at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group). |
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. |
Molecular Formula |
C19H28N8O2
|
---|---|
Molecular Weight |
400.487
|
Exact Mass |
400.2335
|
Elemental Analysis |
C, 56.98; H, 7.05; N, 27.98; O, 7.99
|
CAS # |
1059070-10-8
|
Appearance |
Solid powder
|
SMILES |
O=C1NC2=C(N)N=C(NCCCC)N=C2N1CC3=CC=C(OCCN(C)C)N=C3
|
InChi Key |
SSZHESNDOMBSRV-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C19H28N8O2/c1-4-5-8-21-18-24-16(20)15-17(25-18)27(19(28)23-15)12-13-6-7-14(22-11-13)29-10-9-26(2)3/h6-7,11H,4-5,8-10,12H2,1-3H3,(H,23,28)(H3,20,21,24,25)
|
Chemical Name |
6-Amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]-3-pyridinyl]methyl]-7,9-dihydro-8H-purin-8-one
|
Synonyms |
DSR6434 DSR 6434 DSR-6434
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~125 mg/mL (~312.13 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4969 mL | 12.4847 mL | 24.9694 mL | |
5 mM | 0.4994 mL | 2.4969 mL | 4.9939 mL | |
10 mM | 0.2497 mL | 1.2485 mL | 2.4969 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.