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AS2863619
🥰Excellent
Catalog No. T8378Cas No. 2241300-51-4
AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8/19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector/memory T cells into Foxp3+ regulatory T cells to study various immune diseases.
AS2863619
🥰Excellent
Purity: 100%
Catalog No. T8378Cas No. 2241300-51-4
AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8/19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector/memory T cells into Foxp3+ regulatory T cells to study various immune diseases.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $133 | In Stock | |
| 2 mg | $189 | In Stock | |
| 5 mg | $289 | In Stock | |
| 10 mg | $455 | In Stock | |
| 25 mg | $753 | In Stock | |
| 50 mg | $1,060 | In Stock | |
| 100 mg | $1,430 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $318 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8/19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector/memory T cells into Foxp3+ regulatory T cells to study various immune diseases. |
| Targets&IC50 | CDK19:4.28 nM , CDK8:0.61 nM |
| In vitro | METHODS: Mouse CD4 T cells were treated with AS2863619 (1 μM; 22 hours), and the possible effects of AS2863619 on STAT5 phosphorylation during Foxp3 induction in Tconv cells were investigated. RESULTS AS2863619 inhibited the PSP motif serine phosphorylation of STAT5b to about 40%, while increasing the tyrosine phosphorylation of the C-terminal domain to about 160%; the inhibitory effect of AS2863619 on STAT5b serine phosphorylation was dose-dependent with Foxp3 induction. [1] |
| In vivo | METHODS: Mice were orally treated with AS2863619 (3, 10, or 30 mg/kg). Plasma samples were collected from mice at 1, 2, 4, 8, and 24 hours after administration, and drug levels were determined by high-performance liquid chromatography-tandem mass spectrometry. RESULTS Compared with control mice, AS2863619 treatment after 2,4-dinitrofluorobenzene (DNFB) sensitization suppressed the extent of secondary responses, with less inflammatory cell infiltration into the skin and a lower proportion of interferon-γ (IFN-γ) cells in regional lymph nodes; depletion of Tregs abolished AS2863619-induced suppression before the induction of secondary responses. [1] |
| Molecular Weight | 405.24 |
| Formula | C16H14Cl2N8O |
| Cas No. | 2241300-51-4 |
| Smiles | Cl.Cl.Cc1nc2ccc(cc2[nH]1)-n1c(nc2cnccc12)-c1nonc1N |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 245 mg/mL (604.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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