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| Targets |
LHC-165 targets Toll-like receptor 7 (TLR7), a member of the Toll-like receptor family that plays a critical role in the innate immune system. TLR7 is a pattern recognition receptor that recognizes single-stranded RNA and is primarily expressed in plasmacytoid dendritic cells and B cells. Activation of TLR7 triggers a signaling cascade that leads to the production of pro-inflammatory cytokines and type I interferons, which are essential for antiviral and antitumor immune responses. By acting as a TLR7 agonist, LHC-165 activates the immune system and has the potential to enhance antitumor immunity. The compound is an immuno-oncology modulator that can trigger immune responses against tumors.
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| ln Vitro |
LHC-165 demonstrates potent in vitro activity as a TLR7 agonist. The compound activates TLR7 signaling in immune cells, leading to the production of pro-inflammatory cytokines and type I interferons. Its activity is concentration-dependent, with potent activation observed at appropriate concentrations. LHC-165 has the potential to be studied for the treatment of solid tumors. The compound's activity has been characterized in various cell-based systems using immune cells expressing TLR7. Its potency and selectivity for TLR7 make it a valuable tool for studying TLR7 biology and evaluating TLR7 agonists as immunotherapies for cancer.
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| ln Vivo |
In vivo, LHC-165 has been studied for its potential to treat solid tumors. As a TLR7 agonist, the compound activates the immune system and has the potential to enhance antitumor immunity. TLR7 activation triggers the release of cytokines that can promote antitumor immune responses. Comprehensive in vivo efficacy data for LHC-165 have been reported in research publications. The compound's ability to activate the immune system in vivo makes it a promising candidate for cancer immunotherapy research. Its pharmacokinetic properties support its use in preclinical studies.
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| Enzyme Assay |
In vitro receptor binding assays for LHC-165 involve measuring binding affinity to TLR7. Membranes from cells expressing TLR7 are incubated with a radiolabeled TLR7 ligand and varying concentrations of the test compound. Bound and free radioligand are separated by filtration, and radioactivity is measured. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. Functional assays can measure TLR7 activation by assessing downstream signaling, such as NF-kappaB activation or cytokine production. Cells expressing TLR7 are treated with varying concentrations of the compound, and cytokine levels (e.g., IFN-alpha, IL-6, TNF-alpha) are measured by ELISA. EC50 values are calculated from dose-response curves. Each concentration is typically tested in duplicate or triplicate.
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| Cell Assay |
In vitro cellular assays for LHC-165 are performed using immune cells that express TLR7, such as plasmacytoid dendritic cells, peripheral blood mononuclear cells (PBMCs), or TLR7-expressing cell lines. Cells are treated with varying concentrations of the compound for defined time periods. Cytokine production (IFN-alpha, IL-6, TNF-alpha, IL-12) is measured by ELISA or multiplex bead-based assays. TLR7 signaling activation is assessed by measuring NF-kappaB activation using reporter assays or by Western blot for phosphorylated signaling intermediates. Cell activation markers (CD80, CD86, MHC class II) are measured by flow cytometry. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. EC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for LHC-165 are conducted using mouse models of solid tumors. Immunocompetent mice are implanted with syngeneic tumor cells, and once tumors reach a predetermined size, animals are randomized into treatment groups. LHC-165 is administered via oral gavage, intraperitoneal injection, or subcutaneous injection at various doses and schedules. Tumor growth is measured using calipers. Immune cell infiltration into tumors is assessed by flow cytometry or immunohistochemistry. Cytokine levels are measured in serum and tumor tissues. Pharmacokinetic studies assess drug concentrations in plasma and tissues. Animals are monitored for clinical signs and body weight. Efficacy is expressed as tumor growth inhibition and immune activation compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LHC-165 have been characterized in preclinical studies. The compound has a molecular formula of C29H32F2N3O7P and a molecular weight of 603.55 g/mol. Its chemical name is 3-(5-amino-2-(4-(2-(3,3-difluoro-3-phosphonopropoxy)ethoxy)-2-methylphenethyl)benzo[f][1,7]naphthyridin-8-yl)propanoic acid. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of cancer immunotherapy. Detailed pharmacokinetic data are available from research publications.
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| Toxicity/Toxicokinetics |
LHC-165 is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As a TLR7 agonist that activates the immune system, the compound would be expected to have effects on immune function and could potentially cause cytokine release syndrome or other immune-related adverse events. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound is not approved for human use and is strictly intended for research purposes.
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| References | |
| Additional Infomation |
LHC165, a TLR7 agonist, is a benzonaphthyl Toll-like receptor (TLR) 7 agonist that adsorbs onto aluminum hydroxide and possesses immunostimulatory and potential antitumor activity. Following intratumoral injection of LHC165, the drug is slowly released, targeting, binding to, and activating TLR7. Among other possible responses, this may trigger activation of CD8+ T cells and natural killer (NK) cells, blockade of regulatory T cell (Treg) suppression, and production of interferon-alpha (IFNα). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and innate immune activation.
LHC-165 is a potent Toll-like receptor 7 (TLR7) agonist. It is an immuno-oncology modulator that triggers immune responses against tumors. LHC-165 has the potential to be studied for the treatment of solid tumors. The compound has a molecular formula of C29H32F2N3O7P and a molecular weight of 603.55 g/mol. LHC-165 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. LHC-165 is a valuable research tool for studying TLR7 biology and developing new cancer immunotherapies. |
| Molecular Formula |
C29H32F2N3O7P
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| Molecular Weight |
603.550855636597
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| Exact Mass |
603.194
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| CAS # |
1258595-14-0
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| PubChem CID |
49838259
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
42
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| Complexity |
928
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| Defined Atom Stereocenter Count |
0
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| SMILES |
P(C(CCOCCOC1C=CC(=C(C)C=1)CCC1=CN=C2C(N)=NC3C=C(C=CC=3C2=C1)CCC(=O)O)(F)F)(=O)(O)O
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| InChi Key |
SDLWKRZBLTZSEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H32F2N3O7P/c1-18-14-22(41-13-12-40-11-10-29(30,31)42(37,38)39)7-6-21(18)5-2-20-15-24-23-8-3-19(4-9-26(35)36)16-25(23)34-28(32)27(24)33-17-20/h3,6-8,14-17H,2,4-5,9-13H2,1H3,(H2,32,34)(H,35,36)(H2,37,38,39)
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| Chemical Name |
3-[5-amino-2-[2-[4-[2-(3,3-difluoro-3-phosphonopropoxy)ethoxy]-2-methylphenyl]ethyl]benzo[f][1,7]naphthyridin-8-yl]propanoic acid
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| Synonyms |
LHC-165 LHC165 LHC 165
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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 (e.g. under nitrogen), 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) |
1M NaOH : 50 mg/mL (~82.84 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 | 1.6569 mL | 8.2843 mL | 16.5686 mL | |
| 5 mM | 0.3314 mL | 1.6569 mL | 3.3137 mL | |
| 10 mM | 0.1657 mL | 0.8284 mL | 1.6569 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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