| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
STING (Stimulator of Interferon Genes). STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA is a STING agonist. As an active scaffold, it is designed to activate the STING pathway, triggering innate immune responses. This activation leads to the production of type I interferons and pro-inflammatory cytokines, which promote anti-tumor immunity.
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| ln Vitro |
STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA activates the STING pathway, inducing the expression of type I interferons and other cytokines. As an active scaffold, its biological activity is intrinsic to the STING agonist motif. When conjugated to an antibody, the resulting immune-stimulating antibody conjugate (ISAC) can activate STING selectively in targeted cells.
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| ln Vivo |
In vivo, STING agonists conjugated to tumor-targeting antibodies via scaffolds like STING agonist-20-Ala-amide-PEG2-C2-NH2 have been shown to activate STING within the tumor microenvironment, promoting anti-tumor immune responses. The PEG2 linker provides flexibility and solubility. The C2-NH2 terminus allows for conjugation to antibodies or other targeting moieties.
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| Enzyme Assay |
Not applicable. The compound is intended for use in bioconjugation and is not directly tested in non-cellular binding assays. STING binding can be confirmed using SPR or thermal shift assays with purified STING protein.
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| Cell Assay |
Cell-based STING activation assay: A STING reporter cell line (e.g., THP1-Dual) is seeded in 96-well plates. STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA (0.1-1000 nM) is added directly or conjugated to an antibody that binds to a cell surface receptor. After 18-24 h of incubation at 37degC, reporter activity (IRF-induced SEAP or luciferase) is measured. EC50 values are calculated by non-linear regression.
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| Animal Protocol |
Tumor xenograft model with ISAC: Mice bearing tumor xenografts expressing a specific tumor antigen are administered an ISAC (immune-stimulating antibody conjugate) synthesized from STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA, at doses of 1-10 mg/kg (i.v., once weekly for 2-3 weeks). Tumor volume is measured twice weekly. Serum cytokine levels (IFN-beta, IL-6, TNF-alpha) are measured by ELISA to confirm STING activation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for the free scaffold are not applicable, as it is designed for conjugation to antibodies. When conjugated to an antibody, the PK of the ISAC is dominated by the antibody (half-life of several days to weeks). The PEG2-C2-NH2 linker is stable in circulation and cleaved upon internalization into target cells.
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| Toxicity/Toxicokinetics |
Toxicity data for STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA alone are not available. When conjugated into an ISAC, potential toxicities include cytokine release syndrome (fever, hypotension) and dose-limiting inflammatory responses due to STING activation. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA is a research compound that has not entered clinical trials or received regulatory approval. It is an active scaffold for the synthesis of immune-stimulating antibody conjugates (ISACs), a novel class of targeted immunotherapies. Molecular formula: C48H58F3N13O14; MW: 1098.05. For research use only.
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| Molecular Formula |
C48H58F3N13O14
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|---|---|
| Molecular Weight |
1098.05
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| Related CAS # |
STING agonist-20-Ala-amide-PEG2-C2-NH2;2720500-49-0
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| Appearance |
White to light yellow solid powder
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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 :~100 mg/mL (~91.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.28 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 25.0 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 | 0.9107 mL | 4.5535 mL | 9.1071 mL | |
| 5 mM | 0.1821 mL | 0.9107 mL | 1.8214 mL | |
| 10 mM | 0.0911 mL | 0.4554 mL | 0.9107 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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