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AS2863619 free base

Name: AS2863619 free base
Brand: TargetMol
SKU: T10382
Rating: 4.5 (1 reviews)

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Catalog No. T10382Cas No. 2241300-50-3

AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.

AS2863619 free base

😃Good

Catalog No. T10382Cas No. 2241300-50-3

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$987	6-8 weeks	6-8 weeks
50 mg	$1,360	6-8 weeks	6-8 weeks
100 mg	$1,860	6-8 weeks	6-8 weeks
1 mL x 10 mM (in DMSO)	$381	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Product Introduction

Bioactivity

Description	AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
Targets&IC50	GSK-3α:76.67 nM, GSK-3β:63.06 nM, STAT5:, CDK8:0.61 nM, CDK19:4.28 nM
In vitro	AS2863619 (1 μM; 22 hours; mouse CD4+ T cells) treatment reduces serine phosphorylation of the PSP motif of STAT5b to ~40% and increases tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples.
In vivo	AS2863619 (30 mg/kg; p.o.; daily; for 2 weeks; mice) treatment after sensitization with DNFB dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of IFN-γ+ cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. Treg depletion before the elicitation of the secondary response abolishes AS2863619-induced suppression. KLRG1+ Foxp3+ T cells are specifically increased in DNFB sensitized AS2863619-treated mice.

Chemical Properties

Molecular Weight	332.32
Formula	C₁₆H₁₂N₈O
Cas No.	2241300-50-3
Smiles	Cc1nc2ccc(cc2[nH]1)-n1c(nc2cnccc12)-c1nonc1N
Relative Density.	1.75 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (752.29 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (9.93 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0091 mL	15.0457 mL	30.0915 mL	150.4574 mL
5 mM	0.6018 mL	3.0091 mL	6.0183 mL	30.0915 mL
10 mM	0.3009 mL	1.5046 mL	3.0091 mL	15.0457 mL
20 mM	0.1505 mL	0.7523 mL	1.5046 mL	7.5229 mL
50 mM	0.0602 mL	0.3009 mL	0.6018 mL	3.0091 mL
100 mM	0.0301 mL	0.1505 mL	0.3009 mL	1.5046 mL

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc