| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
When mouse CD4+ T cells were treated with AS2863619 (1 μM) for 22 hours, the amount of serine phosphorylation of the STAT5b PSP motif was reduced to around 40%, whereas the amount of tyrosine phosphorylation of the C-terminal domain was increased to about 160% of the samples treated with control. %[1].
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| ln Vivo |
AS2863619 (30 mg/kg; oral; daily; for 2 weeks; mice) Treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) inhibits the extent of secondary reactions and infiltration of inflammatory cells into the skin Less severe and reduced ratio of changes in interferon-gamma+ (IFN-γ+) cells in a skin contact hypersensitivity model compared to vehicle-treated control mice. Eliminating Tregs before evoking secondary responses eliminated AS2863619-induced suppression. KLRG1+ Foxp3+ T cells were specifically enhanced in DNFB-sensitized AS2863619-treated animals [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Mouse CD4+ T cells Tested Concentrations: 1 μM Incubation Duration: 22 hrs (hours) Experimental Results: Inhibited the serine phosphorylation of the PSP motif of STAT5b to approximately 40%, while inhibiting the tyrosine phosphorylation of the PSP motif of STAT5b to about 40%, while inhibiting the tyrosine phosphorylation of the PSP motif of STAT5b. Amino acid phosphorylation was enhanced to approximately 160% of the control treated sample. |
| Animal Protocol |
Animal/Disease Models: DNFB-induced contact skin allergy in mice [1]
Doses: 30 mg/kg Route of Administration: oral; daily; lasting for 2 weeks Experimental Results: secondary reaction degree, inflammatory cells infiltration into the skin was light, interferon diminished proportion of -γ+ (IFN-γ+) cells. |
| References |
[1]. Akamatsu M, et al. Conversion of antigen-specific effector/memory T cells into Foxp3-expressing Treg cells by inhibition of CDK8/19. Sci Immunol. 2019 Oct 25;4(40). pii: eaaw2707.
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| Molecular Formula |
C16H12N8O
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|---|---|
| Molecular Weight |
332.319480895996
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| CAS # |
2241300-50-3
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| Related CAS # |
AS2863619;2241300-51-4
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O1N=C(C(C2=NC3C=NC=CC=3N2C2=CC=C3C(=C2)NC(C)=N3)=N1)N
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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) |
DMSO : ~250 mg/mL (~752.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.26 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 (6.26 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 (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0091 mL | 15.0457 mL | 30.0915 mL | |
| 5 mM | 0.6018 mL | 3.0091 mL | 6.0183 mL | |
| 10 mM | 0.3009 mL | 1.5046 mL | 3.0091 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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