CL264 |
| Catalog No.GC39361 |
CL264 is a a potent and highly specific toll-like receptor 7 (TLR7) ligand.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1510712-69-2
Sample solution is provided at 25 µL, 10mM.
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CL264 is a a potent and highly specific toll-like receptor 7 (TLR7) ligand. Immune cells utilize toll-like receptors (TLRs) to sense pathogen associated molecular patterns (PAMPs), which represents the starting point of the innate immune response s[1].
Using concentrations from 0.5 to 10 µg/mL, stimulation with CL264 resulted in a dose-dependent secretion of TNF-α after 6 hours. CAL-1 cells were stimulated with CL264 (5 µg/mL) for up to 12 hours. CAL-1 cells were seeded into 96-well plates. After overnight resting, cells were stimulated with CL264 or 9.2s RNA or the combination of both. After incubation as indicated, cell supernatant was analyzed for TNF-α, IL-6, and IFN-β by ELISA. CL264 led to a robust, time-dependent release of TNF-α reaching absolute levels of 1347 pg/mL TNF-α into the supernatant[1].Peripheral blood mononuclear cells (PBMCs) stimulated with CL264, IL-6, IL-8 and IL-12 were significantly stimulated[2].
The TLR7 agonist CL264 ,40 μg/injectionat day 0, 3 and 6 after tumor grafting, stimulated tumor growth, and this pro-tumorigenic effect was completely lost in the absence of MDSCs, both in WT mice and in TLR7 KO mice. The tumor growth exacerbating effect of TLR7 stimulation is mediated by the increased number of MDSCs within the tumor microenvironment.The secretion of CCL2 and GM-CSF by tumor cells was confirmed in vitro, which was found increased in supernatants of CL264-stimulated cells,these results suggest that CL264 may stimulate the recruitment of MDSCs via the induction of CCL2 and GM-CSF.[3].
References:
[1].Hilbert T, Steinhagen F, et al. Synergistic Stimulation with Different TLR7 Ligands Modulates Gene Expression Patterns in the Human Plasmacytoid Dendritic Cell Line CAL-1. Mediators Inflamm. 2015;2015:948540.
[2].Dajon M, Iribarren K, et al. Toll like receptor 7 expressed by malignant cells promotes tumor progression and metastasis through the recruitment of myeloid derived suppressor cells. Oncoimmunology. 2018 Oct 11;8(1):e1505174.
| Cell experiment [1]: | |
Cell lines | Lewis lung carcinoma (LLC),Bone marrow derived macrophages(BMSMs) |
Preparation Method | Macrophages were cultivated in the presence or absence of CL264 for 24 h, before tumor cells were added and co-cultured for 42 h. Radiolabeled thymidine was used to detect tumor cell growth and was added to the co-cultures 18 h before cell harvest. |
Reaction Conditions | Macrophages,CL264(40ng/ml),LLC co-cultured for 42 h |
Applications | CL264 stimulating the BMDMs and it resulted in inhibition of LLC cells, but only when it was used together with IFN-γ. |
| Animal experiment [2]: | |
Animal models | ild-type C57Bl/6J mice,TLR7 Knock out C57Bl/6J mice |
Preparation Method | Cancer cells - Murine lung adenocarcinoma LLC-luc cells (1E6 in 100μl PBS/injection) were injected into the flank of recipient mice. Mice then received intra-tumor injections of CL264 at day 0, 3 and 6 after tumor grafting. |
Dosage form | 40μg/injection, intra-tumor injection |
Applications | Intratumoral injection of the TLR7 agonist CL264 induced a pro-tumorigenic effect.CL264 in TLR7 KO mice, similar to that observed in WT mice.These results clearly demonstrate that the pro-tumorigenic effect of CL264 effect is mediated by an effect on TLR7 expressed by malignant (rather than immune) cells. |
References: | |
| Cas No. | 1510712-69-2 | SDF | |
| Canonical SMILES | O=C(O)CNC(C1=CC=C(CN2C(NC3=C(N)N=C(NCCCC)N=C23)=O)C=C1)=O | ||
| Formula | C19H23N7O4 | M.Wt | 413.43 |
| Solubility | DMSO : 25 mg/mL (60.47 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4188 mL | 12.0939 mL | 24.1879 mL |
| 5 mM | 0.4838 mL | 2.4188 mL | 4.8376 mL |
| 10 mM | 0.2419 mL | 1.2094 mL | 2.4188 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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