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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 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 |
Type I interferons and proinflammatory cytokines are activated in vivo in a STING-dependent manner by subcutaneous injection of diABZI STING agonist-1 triHClide (2.5 mg/kg) [1]. Trihydrochloride diABZI STING Agonist-1 (iv; 3 mg/kg) produced systemic concentrations higher than the half-maximal effective concentration (EC50) of mouse STING (200 ng/ml) and showed systemic exposure with a half-life of 1.4 hours [1]. Eight mice were participated in the trial, which terminated on day 43 [1]. diABZI STING Agonist-1 Trihydrochloride (IV; 1.5 mg/kg; Days 1, 4, and 8; Day 43) dramatically decreased tumor growth and considerably enhanced survival (P < 0.001).
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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: Secretion of IFNβ, IL-6, TNF and CXCL1 in wild-type mice is activated, but not in Sting−/− mice. Animal/Disease Models: BALB/c mouse colorectal tumor syngeneic mouse model (CT-26) [1] Doses: 3 mg/kg Route of Administration: intravenous (iv) (iv)injection; 200mg/kg. 3 mg/kg Experimental Results: The half-life is 1.4 hrs (hrs (hours)), and the systemic concentration is higher than the EC50 of mouse STING (200 ng/ml). 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; 200mg/kg. 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 |
C42H54CL3N13O7
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Molecular Weight |
959.320065021515
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CAS # |
2138299-34-8
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Related CAS # |
diABZI STING agonist-1;2138299-33-7;diABZI STING agonist-1 (Tautomerism);2138498-18-5
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SMILES |
Cl.Cl.Cl.O1CCN(CC1)CCCOC1=CC(C(N)=O)=CC2=C1N(C(NC(C1=CC(C)=NN1CC)=O)=N2)CC=CCN1C(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, 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 : ~90 mg/mL (~93.82 mM)
H2O : ~25 mg/mL (~26.06 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.17 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 20.8 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: ≥ 2.08 mg/mL (2.17 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (34.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.0424 mL | 5.2120 mL | 10.4241 mL | |
5 mM | 0.2085 mL | 1.0424 mL | 2.0848 mL | |
10 mM | 0.1042 mL | 0.5212 mL | 1.0424 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.