| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
CDK8 0.61 nM (IC50) CDK19 4.28 nM (IC50) GSK3α 76.67 nM (IC50) GSK3β 63.06 nM (IC50) STAT5
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|---|---|
| ln Vitro |
Treatment with AS2863619 (1 μM; 22 hours; mouse CD4+ T cells) reduces serine phosphorylation of STAT5b's PSP motif to around 40% while increasing tyrosine phosphorylation in the C-terminal domain to approximately 160% of control-treated samples[1].
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| ln Vivo |
After sensitization to 2,4-dinitrofluorobenzene (DNFB), mice treated with AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks) showed reduced levels of secondary response, milder infiltration of inflammatory cells into the skin, and lower ratios of interferon-γ+ (IFN-γ+) cells in a skin contact hypersensitivity model when compared to vehicle-treated control mice. AS2863619-induced suppression is eliminated by treg depletion prior to the subsequent reaction being elicited. Mice treated with AS2863619 and sensitized to DNFB exhibit a particular increase in KLRG1+ Foxp3+ T cells[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: Suppressed serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples. |
| Animal Protocol |
Animal/Disease Models: Mice with DNFB-induced contact skin hypersensitivity[1]
Doses: 30 mg/kg Route of Administration: Oral administration; daily; for 2 weeks Experimental Results: The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and diminished ratios of interferon-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 |
C16H14CL2N8O
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|---|---|
| Molecular Weight |
405.24
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| CAS # |
2241300-51-4
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| Related CAS # |
AS2863619 free base;2241300-50-3
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| SMILES |
O1N=C(C(C2=NC3C=NC=CC=3N2C2C=CC3=C(C=2)NC(C)=N3)=N1)N.Cl.Cl
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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 : 250 mg/mL (616.92 mM)
H2O : ≥ 100 mg/mL (246.77 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.62 mg/mL (6.47 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.62 mg/mL (6.47 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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: ≥ 2.25 mg/mL (5.55 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. Solubility in Formulation 4: ≥ 2.25 mg/mL (5.55 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 22.5 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. Solubility in Formulation 5: ≥ 2.25 mg/mL (5.55 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 22.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4677 mL | 12.3384 mL | 24.6767 mL | |
| 5 mM | 0.4935 mL | 2.4677 mL | 4.9353 mL | |
| 10 mM | 0.2468 mL | 1.2338 mL | 2.4677 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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