| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
1V209 primarily targets Toll-like receptor 7 (TLR7), a pattern recognition receptor involved in the innate immune response. TLR7 recognizes single-stranded RNA and triggers signaling pathways that lead to the production of pro-inflammatory cytokines and type I interferons. By acting as a TLR7 agonist, 1V209 activates immune cells such as dendritic cells and macrophages, promoting anti-tumor immune responses. The compound can be conjugated to polysaccharides to modulate its pharmacokinetic and pharmacodynamic properties.
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| ln Vitro |
Treatment with 1V209 (0.1–10 μM) dramatically increases TNFα production in RAW246.7 cells[1]. Treatment with 1V209 (18 hours) enhances IL-6 production in dendritic cells generated from bone marrow[1].
In vitro, 1V209 functions as a potent TLR7 agonist. 1V209-polysaccharide conjugates, but not 1V209 alone, increase TNF-α secretion from RAW 264.7 macrophages and IL-6 secretion from bone marrow-derived dendritic cells (BMDCs), with EC50 values ranging from 4.62-61.7 nM and 3.2-188 nM, respectively. These results demonstrate that conjugation to polysaccharides is required for optimal immune activation. The compound shows anti-tumor activity in various in vitro models. |
| ln Vivo |
When the formulation is given intravenously (IV) to mice with 4T1 breast cancer tumors, the animals exhibit less primary tumor development, an accumulation of nanoparticles in the tumors, and an inhibition of lung metastases when compared to the saline-treated mice. At two hours after intravenous injection, mice given 1V209 had significantly higher plasma levels of the proinflammatory cytokines IL-6, IP-10, and MCP-1[1].
In vivo, 1V209 exhibits anti-tumor activity through TLR7-mediated immune activation. Polysaccharide conjugates of 1V209 improve water solubility and enhance efficacy while maintaining low systemic toxicity. The compound has been investigated in various tumor models where TLR7 activation promotes anti-tumor immune responses. In vivo studies demonstrate that 1V209 conjugates can activate the immune system to inhibit tumor growth. The compound's ability to be conjugated to various carriers allows for flexible formulation strategies. |
| Enzyme Assay |
The cell-free assay for 1V209 involves evaluating its binding affinity to TLR7 using surface plasmon resonance (SPR) or similar biophysical techniques. TLR7 protein is typically immobilized on a sensor chip, and 1V209 is flowed over the surface at varying concentrations to determine binding kinetics (ka, kd) and affinity (KD). Competitive binding assays using radiolabeled or fluorescently labeled TLR7 ligands can also be used to determine IC50 values. These assays help characterize the molecular interaction between 1V209 and its target receptor.
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| Cell Assay |
For in vitro cellular assays, 1V209 and its polysaccharide conjugates are tested on immune cells such as RAW 264.7 macrophages and bone marrow-derived dendritic cells (BMDCs). Cells are treated with various concentrations of 1V209 or its conjugates for defined periods. Cytokine secretion (TNF-α, IL-6) is measured using ELISA or multiplex assays. Cell viability is assessed to determine any cytotoxic effects. Dose-response curves are generated to calculate EC50 values for cytokine induction.
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| Animal Protocol |
In vivo animal studies for 1V209 are typically conducted in mouse tumor models. The compound or its polysaccharide conjugates are administered via various routes including intravenous, subcutaneous, or intraperitoneal injection. Tumor growth is monitored by measuring tumor volume using calipers. Immune cell infiltration and activation in tumors are assessed by flow cytometry and immunohistochemistry. Cytokine levels in serum and tumor tissues are measured to evaluate immune activation. Efficacy is evaluated by comparing tumor growth rates and survival between treatment and control groups.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 1V209 include a molecular weight of 359.34 g/mol and molecular formula C16H17N5O5. The compound has a purity of ≥98% and is soluble in DMSO (10 mg/ml) and DMF (0.1 mg/ml). It has a λmax of 285 nm. When conjugated to polysaccharides, the solubility and pharmacokinetic profile of 1V209 are significantly improved. The compound is stored at -20°C and shipped at room temperature.
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| Toxicity/Toxicokinetics |
The toxicity profile of 1V209 is favorable when conjugated to polysaccharides, as this formulation maintains low systemic toxicity. The compound itself shows limited toxicity in preclinical studies. Standard toxicology studies would include assessment of body weight changes, organ histopathology, and clinical chemistry parameters in rodent models. As a TLR7 agonist, potential immune-related toxicities such as cytokine release syndrome should be monitored. 1V209 is intended for research use only and not for therapeutic applications in humans.
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| References | |
| Additional Infomation |
1V209 is a benzoic acid-modified purine TLR7 agonist with anti-tumor activity. It can be conjugated to polysaccharides to improve water solubility, enhance efficacy, and maintain low systemic toxicity. Polysaccharide conjugates of 1V209 increase TNF-α secretion from RAW 264.7 macrophages and IL-6 secretion from BMDCs (EC50s = 4.62-61.7 and 3.2-188 nM, respectively). The compound is a research tool for cancer immunotherapy and has not entered clinical trials. 1V209 is strictly for research purposes and not for therapeutic use in humans.
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| Molecular Formula |
C16H17N5O5
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|---|---|
| Molecular Weight |
359.336683034897
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| Exact Mass |
359.12
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| Elemental Analysis |
C, 53.48; H, 4.77; N, 19.49; O, 22.26
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| CAS # |
1062444-54-5
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| Related CAS # |
1062444-54-5;
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| PubChem CID |
58019867
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| Appearance |
Off-white to yellow solid powder
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COCCOC1=NC(=C2C(=N1)N(C(=O)N2)CC3=CC=C(C=C3)C(=O)O)N
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| InChi Key |
ATISKRYGYNSRNP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17N5O5/c1-25-6-7-26-15-19-12(17)11-13(20-15)21(16(24)18-11)8-9-2-4-10(5-3-9)14(22)23/h2-5H,6-8H2,1H3,(H,18,24)(H,22,23)(H2,17,19,20)
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| Chemical Name |
4-[[6-amino-2-(2-methoxyethoxy)-8-oxo-7H-purin-9-yl]methyl]benzoic acid
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| Synonyms |
1V209 1V-209
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~231.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.79 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (5.79 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 20.8 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 | 2.7829 mL | 13.9144 mL | 27.8288 mL | |
| 5 mM | 0.5566 mL | 2.7829 mL | 5.5658 mL | |
| 10 mM | 0.2783 mL | 1.3914 mL | 2.7829 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.
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