AS2863619

Name: AS2863619
Brand: MedChemExpress
SKU: HY-126675A
Rating: 5.0 (2 reviews)

Cat. No.: HY-126675A Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3⁺ regulatory T (T_reg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC₅₀s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.

For research use only. We do not sell to patients.

AS2863619 Chemical Structure

CAS No. : 2241300-51-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 385	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 385	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 166	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of AS2863619:

AS2863619 free base Get quote

2 Publications Citing Use of MCE AS2863619

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•Related Screening Libraries:

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View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

View All STAT Isoform Specific Products:

View All Isoforms

STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK8

0.61 nM (IC₅₀)

CDK19

4.28 nM (IC₅₀)

GSK3α

76.67 nM (IC₅₀)

GSK3β

63.06 nM (IC₅₀)

STAT5

In Vitro

AS2863619 (1 μM; 22 hours; mouse CD4⁺ T cells) treatment suppresses 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	Mouse CD4⁺ T cells
Concentration:	1 μM
Incubation Time:	22 hours
Result:	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.

In Vivo

AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ⁺ (IFN-γ⁺) cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. T_reg 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice with DNFB-induced contact skin hypersensitivity^[1]
Dosage:	30 mg/kg
Administration:	Oral administration; daily; for 2 weeks
Result:	The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ⁺ (IFN-γ⁺) cells.

Molecular Weight

405.24

Formula

C₁₆H₁₄Cl₂N₈O

CAS No.

2241300-51-4

Appearance

Solid

Color

White to off-white

SMILES

NC1=NON=C1C(N2C3=CC=C4N=C(C)NC4=C3)=NC5=C2C=CN=C5.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (616.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (246.77 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.62 mg/mL (6.47 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.62 mg/mL (6.47 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.25 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (287 KB) SDS (251 KB)

COA (263 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.4677 mL	12.3384 mL	24.6767 mL	61.6918 mL
	5 mM	0.4935 mL	2.4677 mL	4.9353 mL	12.3384 mL
	10 mM	0.2468 mL	1.2338 mL	2.4677 mL	6.1692 mL
	15 mM	0.1645 mL	0.8226 mL	1.6451 mL	4.1128 mL
	20 mM	0.1234 mL	0.6169 mL	1.2338 mL	3.0846 mL
	25 mM	0.0987 mL	0.4935 mL	0.9871 mL	2.4677 mL
	30 mM	0.0823 mL	0.4113 mL	0.8226 mL	2.0564 mL
	40 mM	0.0617 mL	0.3085 mL	0.6169 mL	1.5423 mL
	50 mM	0.0494 mL	0.2468 mL	0.4935 mL	1.2338 mL
	60 mM	0.0411 mL	0.2056 mL	0.4113 mL	1.0282 mL
	80 mM	0.0308 mL	0.1542 mL	0.3085 mL	0.7711 mL
	100 mM	0.0247 mL	0.1234 mL	0.2468 mL	0.6169 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

AS2863619 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AS28636192241300-51-4AS 2863619AS-2863619CDKSTATCyclin dependent kinaseInhibitorinhibitorinhibit

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AS2863619

Customer Review

Other Forms of AS2863619:

AS2863619 Related Antibodies

2 Publications Citing Use of MCE AS2863619

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All STAT Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

AS2863619 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AS2863619 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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