| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
diABZI STING agonist-3 is a potent and selective stimulator of interferon genes (STING) receptor agonist with an EC50s of 130 for human PBMCs. It is able to activate STING and stimulate the secretion of IFNβ, IL-6, TNF, and KC/GROα, exhibiting durable anti-tumour effects.
| ln Vitro |
The selective interferon gene (STING) receptor agonist stimulator diABZI STING agonist-1 (tautomer) has EC50 values of 130 and 186 nM for humans and mice, respectively. Compound 3, diABZI STING agonist-1, shows excellent selectivity for more than 350 tested 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 diABZI STING agonist-1 (tautomer) (subcutaneous injection; 2.5 mg/kg) [1]. The diABZI STING Agonist-1 (tautomer) (iv; 3 mg/kg) exhibited a half-life of 1.4 hours for systemic administration and attained systemic concentrations higher than the mouse STING's half-maximum effective concentration (EC50) of 200 ng/ml [1]. By the end of the trial, eight mice remained tumor-free on day 43 after treatment with diABZI STING agonist-1 (tautomer) (iv; 1.5 mg/kg; 43 days) significantly suppressed tumor growth and significantly increased survival (P < 0.001) in 10 mice [1].
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| Animal Protocol |
Animal/Disease Models: wild and Sting−/− C57Blk6 mice
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 this is not the case 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 |
| Molecular Formula |
C42H51N13O7
|
|---|---|
| Molecular Weight |
849.9372
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| Exact Mass |
849.403
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| CAS # |
2138498-18-5
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| Related CAS # |
diABZI STING agonist-1;2138299-33-7;diABZI STING agonist-1 trihydrochloride;2138299-34-8
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| PubChem CID |
131986624
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| Appearance |
White to light yellow solid powder
|
| LogP |
1.9
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
62
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| Complexity |
1570
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C([H])([H])C([H])([H])OC1=C([H])C(C(N([H])[H])=O)=C([H])C2=C1N(C(N([H])C(C1=C([H])C(C([H])([H])[H])=NN1C([H])([H])C([H])([H])[H])=O)=N2)C([H])([H])/C(/[H])=C(\[H])/C([H])([H])N1C(N([H])C(C2=C([H])C(C([H])([H])[H])=NN2C([H])([H])C([H])([H])[H])=O)=NC2C([H])=C(C(N([H])[H])=O)C([H])=C(C1=2)OC([H])([H])[H]
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| InChi Key |
JGLMVXWAHNTPRF-CMDGGOBGSA-N
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| InChi Code |
InChI=1S/C42H51N13O7/c1-6-54-31(19-25(3)49-54)39(58)47-41-45-29-21-27(37(43)56)23-33(60-5)35(29)52(41)12-8-9-13-53-36-30(46-42(53)48-40(59)32-20-26(4)50-55(32)7-2)22-28(38(44)57)24-34(36)62-16-10-11-51-14-17-61-18-15-51/h8-9,19-24H,6-7,10-18H2,1-5H3,(H2,43,56)(H2,44,57)(H,45,47,58)(H,46,48,59)/b9-8+
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| Chemical Name |
1-[(E)-4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-morpholin-4-ylpropoxy)benzimidazol-1-yl]but-2-enyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazole-5-carboxamide
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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.
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