| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
In rat liver triploids, dazostigen (ADC-1, linker-payload) (121 μM; 10 min-24 hr) has a half-life (t1/2 of 2.4 hours [1]. In THP1 cells expressing the R232 variation of human STING, dazostigen (ADC-1, linker-payload) activates human guanylate cyclase C (GCC) at an EC50 of 0.068 nM [1]. In human, primate, and mouse plasma, Dazostinag (ADC-1) (10 μg/mL; 0-96 hours) demonstrates plasma stability [1].
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| ln Vivo |
In tumor-bearing Balb/C mice carrying CT26-GCC, dazostinag (ADC-1) (0.1 mg/kg; single dose) had a half-life of 33 hours and an AUC (last) value of 51432 h·nM[1]. In Balb/C mice and GCC-expressing CT26 colon cancer mice, dazostinag (ADC-1) (50 μg/kg, 100 μg/kg; intravenous injection; single dosage, monitored for 2 weeks) effectively reduces tumor growth[1].
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| Animal Protocol |
Animal/Disease Models: CT26 colon carcinoma model in female balb/c (Bagg ALBino) mouse (6-8 weeks old)[1]
Doses: 50 μg/kg, 100 μg/kg Route of Administration: IP; single dose, monitored for 15 days, measured two times per week Experimental Results: Dramatically suppressed the volume of tumor in mice. |
| References |
| CAS # |
2553413-86-6
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|---|---|
| Related CAS # |
Dazostinag disodium;2553413-93-5
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| Appearance |
Typically exists as solid at room temperature
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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.) |
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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