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CDK8/19-IN-2

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Catalog No. T88262Cas No. 3024381-54-9

CDK8/19-IN-2 (compound 12) is a potent inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), exhibiting IC 50 values of 2.08 nM and 2.49 nM, respectively. This orally active compound is applicable in the research of acute myeloid leukemia (AML), breast cancer, and lymphoma.

CDK8/19-IN-2

CDK8/19-IN-2

😃Good
Catalog No. T88262Cas No. 3024381-54-9
CDK8/19-IN-2 (compound 12) is a potent inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), exhibiting IC 50 values of 2.08 nM and 2.49 nM, respectively. This orally active compound is applicable in the research of acute myeloid leukemia (AML), breast cancer, and lymphoma.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$2,12010-14 weeks10-14 weeks
50 mg$2,78010-14 weeks10-14 weeks
100 mg$3,70010-14 weeks10-14 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
CDK8/19-IN-2 (compound 12) is a potent inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), exhibiting IC 50 values of 2.08 nM and 2.49 nM, respectively. This orally active compound is applicable in the research of acute myeloid leukemia (AML), breast cancer, and lymphoma.
Targets&IC50
CDK8-CyclinC:2.08 nM, CDK19-CyclinC:2.49 nM
In vitro
CDK8/19-IN-2 (compound 12) inhibits the proliferation of MV4-11 human AML cells with an IC 50 of 5.719 nM [1]. Additionally, CDK8/19-IN-2 (at concentrations of 0-10 μM) dose-dependently reduces the phosphorylation of STAT1 at serine 727 (p-STAT1 S727) [1].
In vivo
CDK8/19-IN-2, also known as compound 12, was administered orally at doses of 3-10 mg/kg once daily using gavage in female BALB/c nude mice (6-8 weeks, human AML cell line MV4-11 was subcutaneously inoculated at the right flanks). The compound demonstrated a dose-dependent suppression of tumor growth, achieving tumor growth inhibition (TGI) of 29% and 76% at doses of 3 mg/kg and 10 mg/kg, respectively, without impacting the body weight of the animals [1].
Chemical Properties
Molecular Weight494.17
FormulaC17H20Br2F2N4O
Cas No.3024381-54-9
SmilesFC(F)C=1C(Br)=C(Br)C=C2C1N=C(N2C3CCOCC3)N4CCNCC4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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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
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