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| 5mg |
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| Targets |
AXC-715 is a TLR7/TLR8 dual agonist, targeting both Toll-like receptor 7 and Toll-like receptor 8. These receptors are endosomal pattern recognition receptors expressed primarily on plasmacytoid dendritic cells (pDCs) and myeloid dendritic cells (mDCs), respectively. Activation of TLR7/TLR8 triggers the MyD88-dependent signaling pathway, leading to NF-kappaB and IRF7 activation, which results in the production of pro-inflammatory cytokines (e.g., IL-6, TNF-alpha, IL-12) and type I interferons (e.g., IFN-alpha).
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| ln Vitro |
As a TLR7/TLR8 dual agonist, AXC-715 trihydrochloride promotes cytokine production and dendritic cell activation. It stimulates the release of pro-inflammatory cytokines and type I interferons from immune cells, which in turn promotes the activation and maturation of antigen-presenting cells (APCs), enhances antigen presentation, and drives the differentiation of naive T-cells into effector T-cells. This immune activation is central to its application as an adjuvant in cancer immunotherapy and vaccine development.
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| ln Vivo |
Specific in vivo data for AXC-715 trihydrochloride are not detailed in the literature. However, as a TLR7/TLR8 dual agonist, it is designed to be conjugated to PD-L1-targeting antibodies via antibody-adjuvant immunoconjugate technology. The antibody targets PD-L1-expressing tumor cells or immune cells in the tumor microenvironment, delivering the TLR7/TLR8 agonist directly to the tumor site, where it activates local antigen-presenting cells and promotes anti-tumor immune responses while minimizing systemic toxicity.
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| Enzyme Assay |
AXC-715 trihydrochloride is not a direct enzyme inhibitor; its activity is measured via cell-based functional assays for TLR7 and TLR8 activation. A typical assay uses HEK293 cells stably transfected with human TLR7 or TLR8 and an NF-kappaB-driven luciferase reporter gene. Cells are seeded in 96-well plates and treated with varying concentrations of AXC-715 (0.001-10 microM) for 6-18 hours. Luciferase activity is then measured using a luminometer, and the EC50 for TLR7 and TLR8 activation is calculated from the dose-response curve.
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| Cell Assay |
Cellular activation assays are performed using human peripheral blood mononuclear cells (PBMCs) or isolated dendritic cells. Cells are seeded in 96-well plates and treated with varying concentrations of AXC-715 trihydrochloride (0.01-10 microM) for 24-48 hours. After treatment, culture supernatants are collected, and cytokine levels (IL-6, TNF-alpha, IL-12, IFN-alpha) are measured by ELISA or multiplex bead-based assays. Dendritic cell activation is assessed by flow cytometry measuring upregulation of co-stimulatory markers CD80, CD86, CD83, and MHC class II.
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| Animal Protocol |
In vivo protocols for antibody-adjuvant immunoconjugates (AICs) incorporating AXC-715 are not detailed in the literature. A typical study would use a syngeneic mouse tumor model such as CT26 or MC38. The AXC-715-conjugated PD-L1 antibody is administered via intravenous injection (e.g., 1-10 mg/kg) every 3-7 days for 2-3 weeks. Tumor volume is measured twice weekly. On study termination, tumors are harvested for flow cytometry analysis of immune cell infiltration (dendritic cells, CD8+ T cells, regulatory T cells) and cytokine levels in tumor tissue. Local and systemic cytokine levels in plasma are also measured.
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| ADME/Pharmacokinetics |
Specific PK parameters for AXC-715 trihydrochloride are not detailed. As a small-molecule TLR agonist, it is not typically administered as a free drug but rather conjugated to an antibody via a linker for targeted delivery. When conjugated, the pharmacokinetic properties of the immunoconjugate are governed primarily by the antibody component, resulting in a longer half-life and selective tumor accumulation through the enhanced permeability and retention (EPR) effect and active targeting via PD-L1 binding.
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| Toxicity/Toxicokinetics |
Specific toxicological data for AXC-715 trihydrochloride are not detailed. As a TLR7/TLR8 agonist, systemic administration of the free compound could potentially induce excessive systemic inflammation (cytokine storm), flu-like symptoms, and autoimmune reactions. This is precisely why the compound is designed to be conjugated to a PD-L1-targeting antibody, to restrict its activity to the tumor microenvironment and minimize systemic toxicities. The safety profile of the immunoconjugate is expected to be improved over the free TLR agonist.
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| References | |
| Additional Infomation |
AXC-715 trihydrochloride is a research-grade chemical tool for immune-oncology research. TLR7/TLR8 agonists are known potent inducers of type I interferons and pro-inflammatory cytokines, and they have been explored as cancer immunotherapies and vaccine adjuvants. By conjugating this TLR7/TLR8 dual agonist to a PD-L1 antibody, researchers aim to convert checkpoint blockade therapy into a localized immune-activating therapy that may overcome resistance to checkpoint inhibitors. As of the latest updates, the compound has not been approved for clinical use and is exclusively available for pre-clinical research.
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| Molecular Formula |
C18H28CL3N5
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| Molecular Weight |
420.81
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| Exact Mass |
419.141
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| CAS # |
2479276-17-8
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| Related CAS # |
AXC-715 hydrochloride;2490497-93-1
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| PubChem CID |
155908840
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| Appearance |
White to yellow solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N1C(=NC2C(N)=NC3=CC=CC=C3C1=2)CCCC)CCCN.Cl.Cl.Cl
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| InChi Key |
ZSUHKPUPLPQJGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H25N5.3ClH/c1-2-3-10-15-22-16-17(23(15)12-7-6-11-19)13-8-4-5-9-14(13)21-18(16)20;;;/h4-5,8-9H,2-3,6-7,10-12,19H2,1H3,(H2,20,21);3*1H
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| Chemical Name |
1-(4-aminobutyl)-2-butylimidazo[4,5-c]quinolin-4-amine;trihydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~125 mg/mL (~297.05 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3764 mL | 11.8818 mL | 23.7637 mL | |
| 5 mM | 0.4753 mL | 2.3764 mL | 4.7527 mL | |
| 10 mM | 0.2376 mL | 1.1882 mL | 2.3764 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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