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1mg |
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diABZI STING agonist-1 is a novel, potent and selective STING (stimulator of interferon genes) receptor agonist, with an EC50s of 130 nM for human PBMCs.
ln Vitro |
diABZI STING agonist-1 is a stimulator of the selective interferon gene (STING) receptor having EC50 values of 186 nM for mice and 130 nM for humans, respectively. Compound 3, diABZI STING agonist-1, shows excellent selectivity for more than 350 investigated kinases at 1 μM [1].
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ln Vivo |
In vivo, STING-dependent activation of type I interferons and proinflammatory cytokines is induced by diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) [1]. ? DiABZI STING Agonist-1 (iv; 3 mg/kg) produced systemic concentrations higher than the half-maximum effective concentration (EC50) of mouse STING (200 ng/ml) and showed systemic exposure with a half-life of 1.4 hours [1]. Significantly reducing tumor development and improving survival was the effect of diABZI STING Agonist-1 (iv; 1.5 mg/kg; Days 1, 4, and 8; Day 43). [1].
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Animal Protocol |
Animal/Disease Models: Wild and Sting−/− C57Blk6 mice[1]
Doses: 2.5 mg/kg Route of Administration: subcutaneous injection; 2.5 mg/kg Experimental Results: The secretion of IFNβ, IL-6, TNF and CXCL1 was activated in wild-type mice, but Sting None in −/− mice. BALB/c mouse colorectal tumor syngeneic mouse model (CT-26) [1] Doses: 3 mg/kg Route of Administration: intravenous (iv) (iv)injection; 3 mg/kg Experimental Results: Half-life is 1.4 hrs (hrs (hours)), systemic concentration is greater than the EC50 of mouse STING (200 ng/ Animal/Disease Models: BALB/c mouse colorectal tumor syngeneic mouse model (CT-26) [1] Doses: 1.5 mg/kg Route of Administration: intravenous (iv) (iv)injection; 1.5 mg/kg; 43-day Experimental Results: Dramatically inhibited tumor growth and improved survival rate. |
References |
[1]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7.
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Molecular Formula |
C42H51N13O7
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Molecular Weight |
849.937247514725
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CAS # |
2138299-33-7
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Related CAS # |
diABZI STING agonist-1 trihydrochloride;2138299-34-8;diABZI STING agonist-1 (Tautomerism);2138498-18-5
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SMILES |
O1CCN(CC1)CCCOC1=CC(C(N)=O)=CC2=C1N(C(NC(C1=CC(C)=NN1CC)=O)=N2)C/C=C/CN1C(NC(C2=CC(C)=NN2CC)=O)=NC2C=C(C(N)=O)C=C(C1=2)OC
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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 and light. |
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 (~117.66 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.5 mg/mL (4.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 35.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.5 mg/mL (4.12 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 35.0 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 | 1.1766 mL | 5.8828 mL | 11.7655 mL | |
5 mM | 0.2353 mL | 1.1766 mL | 2.3531 mL | |
10 mM | 0.1177 mL | 0.5883 mL | 1.1766 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.