STING agonist-45
Based on 1 Customer Validation
STING agonist-45 is a selective STING agonist (EC50 = 0.28 μM). STING agonist-45 activates the innate immune response through the cGAS-STING pathway, upregulating key markers such as p-TBK1 and IRF3. STING agonist-45 exhibits robust STING activation in human peripheral blood mononuclear cells (PBMCs), inducing the production of type I interferons (such as IFN-β) and downstream cytokines (such as TNF-α and IL-6). STING agonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8+ T cell infiltration in mouse models. STING agonist-45 is promising for the study of STING-related diseases.
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- Pureté : 99.10%
- CAS No.: 2361424-97-5
- Formule: C21H26N6O4
- Masse moléculaire:426.47
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
STING agonist-45 (Compound 12L) (24 h) induces reporter signal in RAW 264.7 cells with an EC50 value of 5.22 µM [1].
STING agonist-45 (24 h) shows obvious cytotoxicity against THP1 cells[1].
STING agonist-45 (24 h) bind to carboxy terminal domain (CTD) of various hSTING alleles (IC50 = 8.97 µM) and mSTING (IC50 = 4.35 µM)[1].
STING agonist-45 (Example 1) (24 h) stimulates the production of CXCL10 (IP10) cytokines in THP1 cells, with an EC50 value of 1.6 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-t | AUC0-∞ | CL | MRT0-∞ | Vss |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.v. | 1.13 h | 3820 ng·h/mL | 3833 ng·h/mL | 43.8 mL/min/kg | 0.894 h | 2377 mL/kg |
In Vivo
STING agonist-45 (10 mg/kg, i.v., once a day, 7 days) reduces tumor volume, prolongs the survival time in B16.F10 tumor-bearing C57BL/6 mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (6-8 weeks old) model[1]
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Dosage:3, 10, 30 mg/kg
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Administration:i.v., once a day, 4 days
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Result:Dose-dependent induced IFN-β protein.
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Animal Model:B16.F10 tumor-bearing (105) C57BL/6 mice (6-8 weeks old) model[1]
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Dosage:10 mg/kg
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Administration:i.v., once a day, 7 days
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Result:Reduced tumor volume, prolonged the survival time.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2361424-97-5
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Appearance Solid
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Masse moléculaire 426.47
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Formule C21H26N6O4
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Color White to light yellow
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SMILES
O=C(C1=CC2=C(C(OC3COC3)=C1)N(CCC)C(NC(C4=CC(C)=NN4CC)=O)=N2)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (234.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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PBMC Thawing for Immune Assays
PBMC thawing for immune assays recovers viable cryopreserved peripheral blood mononuclear cells for downstream functional or phenotypic readouts, including ELISPOT, intracellular cytokine staining, proliferation assays, and flow-cytometric immunophenotyping. Cryopreserved PBMCs can support immune monitoring because antigen-specific T-cell function and major CD4/CD8 phenotypes may be retained after optimized freezing and thawing, although some lymphocyte subsets and activation or memory markers can be altered by cryopreservation. The technical objective is rapid warming of the frozen vial followed by controlled dilution and removal of DMSO-containing cryomedium, because thawing and wash conditions measurably affect viable PBMC recovery and downstream assay performance. Viability alone is insufficient for protocol evaluation because high viability may occur with low live-cell recovery, so both viable percentage and absolute live-cell recovery should be measured after thawing.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | 58.6208 mL |
| 5 mM | 0.4690 mL | 2.3448 mL | 4.6897 mL | 11.7242 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8621 mL | |
| 15 mM | 0.1563 mL | 0.7816 mL | 1.5632 mL | 3.9081 mL | |
| 20 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9310 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9379 mL | 2.3448 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9540 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4655 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9770 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL |
STING agonist-45 Related Classifications
HY-177338 Related Classifications
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